Research & Reviews: A Journal of Pharmaceutical Science
Research and Reviews: Journal of Pharmaceutical Science (RRJoPS) is a print and eJournal focused towards the rapid publication of fundamental research papers in all areas of Pharmaceutical Sciences. The Journal Intends to publish all recent advancements in the field of Pharmaceutics Focus and Scope covers but is not limited to Basic pharmaceutical sciences Pharmaceutics Pharmacokinetics Pharmaceutical Engineering Pharmaceutical Nanotechnology Pharmaceutical Analysis Biopharmaceutics, Pharmacodynamics Protein-Peptide chemistry Pharmaceutical technology Pharmaceutical Toxicology Pharmaceutical validation techniques Pharmacotherapy Pharmacogenomics Quality Control Drug and Pro-drug design
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A Comprehensive Review on Buccal Drug Delivery System
Buccal delivery involves the running of the desired drug through the buccal mucosal membrane lining of the oral cavity. The buccal region of the oral cavity is a striking target for administration of the drug of choice because it offers some discrete advantages over all other routes. However, the mucosal lining of the oral cavity drugs which undergo rigorous firstpass metabolism, for those drugs, buccal route are excellent. Buccal drug delivery is a potential area for continued research with the aim of systemic delivery of orally ineffective drugs as well as a feasible and striking alternative for non-invasive delivery of potent peptide and protein drug molecules. The buccal formulations are sited in the mouth between the upper gingival (gums) and cheek to treat local and systemic conditions. Bioadhesion is defined as the affirm in which two bodies’ one or both of adherents are of a biological nature and are held mutually for extended periods of time by interfacial forces. A bioadhesive can therefore be distinct as a substance, which has an ability to interact with biological materials, and is capable of being retained on the biological substrate for a period of time. However, the need for safe and effective buccal permeation/absorption enhancers is a vital component for a prospective future in the area of buccal drug delivery. Keywords: Buccal drug delivery, bioadhesion, first pass metabolism, mucoadhesion Ipshita Sarkar, Jaimini Gandhi, Pranav Shah et al. A Comprehensive Review on Buccal Drug Delivery System. Research and Reviews: A Journal of Pharmaceutical Science. 2017; 8(2): 20–32p.
Quantitative Structure Activity Relationship Studies of Some New 4-Thiazolidinone Derivatives as Antimicrobial Agents
In the present study, quantitative structure activity relationship (QSAR) studies have been performed on series of 24 compounds of 4-thiazolidinone derivatives with antimicrobial activity using Chemoffice version 8.0 software. The QSAR models have been developed by using multiple linear regressions in order to identify descriptors, which are actually focusing towards the biological activity. Leave one out (LOO) method was employed in cross validation analysis to validate the developed model. The best predictive QSAR model derived, had r2cv of 0.76, non-cross validated r2 of 0.9, and predictive r2 for test set 0.87. The model reveals that some multidimensional steric factors and electronic factors like HF (heat of formation), PMI-Y (principle moment of inertia-Y axis), D2 (Dipole energy) and electronic energy show strong correlation with biological activity. These models are expected to be useful as antimicrobial agents. Training set was formed by selecting 19 compounds from original series. Test set compounds were selected randomly. The validation techniques utilized in this work illustrate the accuracy and robustness of the constructed model by calculating its fitness on training and test set. Keywords: 4-thiazolidinone antimicrobial agents derivatives, quantitative structure activity relationship, Blessy Jacob, Bisht Lata K, Vineeth Chandy. Quantitative Structure Activity Relationship Studies of Some New 4- Thiazolidinone Derivatives as Antimicrobial Agents. 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Formulation, Optimization and Evaluation of Flurbiprofen Liposomal Gel
The present study deals with effect of various combinations of lecithin, cholesterol, chloroform-methanol and tween-80 on liposomes of flurbiprofen. Optimization of the flurbiprofen liposomes by Design Expert software was done. Vesicle size, drug content, SEM and entrapment efficiency were evaluated. Flurbiprofen gel with optimized liposome using Carbopol 934 as gelling agents, were formulated. pH, spreadability and drug content in the gel were evaluated. Results of skin irritation study showed that formulation is nonirritant. Exvivo release study of flurbiprofen liposomal gel and gel with pure drug were compared using rat abdominal skin. This revealed that liposomal gel have better skin penetration than conventional gel. The kinetics of drug release followed higuchi release with anomalous nonfickian diffusion. The formulation was found to be stable even after accelerated stability study as per ICH guidelines. Keywords: Flurbiprofen, liposomal gel, Box-Behnken design, optimization, ex-vivo release study Cite this Article Arun Raj R, Nikita Sara Abraham. Formulation, Optimization and Evaluation of Flurbiprofen Liposomal Gel. Research & Reviews: A Journal of Pharmaceutical Science. 2016; 8(2): 33–42p.
Two New, Useful and Facile Stability-Indicating UV Spectrophotometric Methods for the Determination of Rosiglitazone in Pharmaceuticals
Rosiglitazone (ROS) is an antidiabetic drug belonging to the thiozolidine class. Two simple, rapid, sensitive, accurate and reproducible UV-spectrophotometric methods were developed and subsequently validated for the determination of ROS in bulk and tablet form. The methods are based on the measurement of the absorbance of the drug solution either in 0.1 M NaOH (NaOH method) or in 0.1 M HCl (HCl method) at 316 nm in both instances. The developed methods were validated for several parameters as per the ICH guidelines. Beer’s law was obeyed over the concentration ranges 4–72 µg ml-1and 2.5–45.0 µg ml-1, for both NaOH and HCl diluents, respectively, with corresponding molar extinction coefficients of 4.61 × 103 and 7.32 × 103 l mol-1 cm-1. The calculated limits of detection (LOD) and limits of quantification (LOQ) were 0.44 and 1.33 µg ml-1 (NaOH method) and 0.28 and 0.86 µg ml-1 (HCl method), respectively. The intraday and interday percent RE values, reflective of accuracy, were <2%; and the methods were also found to be repeatable and reproducible with %RSD values of <2%. Results of robustness and ruggedness were satisfactory. The methods were also shown to be selective as seen from the results of placebo and synthetic mixture analyses. When applied to tablets, results obtained were comparable with the label claim as well as those obtained by a reference method. As part of stress testing, the drug was subjected to forced degradation under the recommended stress conditions of ICH, and it was found to undergo substantial degradation under base hydrolysis and oxidation-induced stress conditions, but remained inert to acid hydrolysis, photolytic- and heat-induced stress conditions, thereby reflecting the stability-indicating ability of the methods. Keywords: Rosiglitazone, determination, UV-spectrophotometry, pharmaceuticals, stabilityindicating Cite this Article Basavaiah K, Rajendraprasad N. Two New, Useful and Facile StabilityIndicating UV Spectrophotometric Methods for the Determination of Rosiglitazone in Pharmaceuticals. Research and Reviews: A Journal of Pharmaceutical Science. 2017; 8(2): 8–19p.
3D QSAR Studies of 2,3-Disubstituted Quinazolin Phenyl Acetic Acid Derivatives as Antimicrobial Agents
Quantitative structure activity relationship (QSAR) studies have been performed on series of 31 compounds of 2,3-disubstituted quinazolin phenyl acetic acid derivatives with antimicrobial activity using Chemoffice version 8.0 software. The QSAR models have been developed by using multiple linear regressions in order to identify descriptors, which are actually focusing towards the biological activity. Leave one out (LOO) method was employed in cross validation analysis to validate the developed model. The best predictive QSAR model derived, had r2cv of 0.88, non-cross validated r2 of 0.9, predictive r2 for test set 0.7 and standard error of estimate 0.3. The model reveals that some multidimensional steric factors and electronic factors like Pc (octonol/water partition coefficient), HOMO (energy of highest occupied molecular orbitals), LUMO (energy of the lowest unoccupied molecular orbitals) and electronic energy show strong correlation with biological activity. These models are expected to be useful as antimicrobial agents. Keywords: QSAR, leave one out, HOMO, LUMO Blessy Jacob, Bisht Lata K, Vineeth Chandy. 3D QSAR Studies of 2,3- Disubstituted Quinazolin Phenyl Acetic Acid Derivatives as Antimicrobial Agents. Research and Reviews: A Journal of Pharmaceutical Science. 2017; 8(2): 4–7p.
Autistic Spectrum Disorder (ASD) is a neurological and developmental disorder that begins early in childhood and last throughout person’s life. It is called spectrum disorder because people with ASD can have a range of symptoms like disabilities in communication, restricted interest and repetitive behavior. Causes: Autism is highly heritable, researchers suspect both environmental and genetic factors as causes. In rare cases, autism is strongly associated with agents that cause birth defects. Sign and Symptoms: Parents usually notice signs in the first two years of their child's life. These signs often develop gradually, though some children with autism reach their developmental milestones at a normal place and then regress. The diagnostic criteria require that symptoms become apparent in early childhood, typically before age three. Treatment: It include behavior and communication therapies, skills training and medicines to control symptoms. Keywords: Autism, genetic, children, echolalic, insomnia Cite this Article Thounaojam Monica. Autism Spectrum Disorder. Research and Reviews: A Journal of Pharmaceutical Science. 2017; 8(1): 10–16p.
Development and Validation of HPTLC Methods for Estimation of Trimebutine Maleate in Pharmaceutical Formulation
A simple and rapid high-performance thin-layer chromatographic (HPTLC) method was developed and validated for quantitative determination of trimebutine maleate in single dose formulation. Trimebutine maleate was chromatographed on silica gel 60 F 254 TLC plate using methanol–toluene (8:2 v/v) as mobile phase. The plates were developed to a distance of 8 cm at ambient temperature. Trimebutine maleate was quantified by densitometric analysis at 271 nm. The method was found to give compact spots for the drug (Rf=0.49± 0.01). The linear regression analysis data for the calibration plots showed good linear relationship with R² = 0.999 in the concentration range 50–300 ng/spot. The method was validated for precision, recovery, repeatability, and robustness as per the International Conference on Harmonization (ICH) guidelines. The minimum detectable amount was found to be 1.18 ng/spot, whereas the limit of quantitation was found to be 3.58 ng/spot. Statistical analysis of the data showed that the method is precise, accurate, reproducible, and selective for the analysis of trimebutine maleate. Keywords: trimebutine maleate, high-performance thin-layer chromatography (HPTLC), validation Cite this Article Bhole RP, Jadhav D, Wankhede SB, et al. Development and Validation of HPTLC Methods for Estimation of Trimebutine Maleate in Pharmaceutical Formulation. Research and Reviews: A Journal of Pharmaceutical Science. 2017; 8(1): 17–22p.
Modified Nucleosides “(ProTide)â€ as Potential Anti-HCV Therapeutics
Hepatitis C virus (HCV) is among the most common causes of cirrhosis and chronic liver disease worldwide. As a result, many researchers are interested in designing and synthesis of a clinical treatment for HCV. Nucleoside monophosphates and monophosphonates play such an important role for treatments of incurable diseases such as hepatitis. For example, 2'-C-methyladenosine and 2'-C-methyl guanosine have shown activities against HCV in the replicon assay as well as against several members of the flavivirus family. However, their development as drug molecules has been hindered by the inherent poor drug-like properties of the monophosphate and monophosphonate groups. These groups have low bioavailability due to the inefficient cellular uptake, poor in vivo stability and poor intracellular metabolism; the latter drawback being most relevant to monophosphates than monophosphonates. These limitations can be addressed by using por Tide strategy, which is able to help the nucleoside monophosphate delivered inside the cell. In this review, we have discussed the different keys monophosphate and monophosphonate nucleoside prodrugs that has entered clinical development. In addition, the role of the ProTide technology is highlighted for the success in the discovery of nucleoside therapeutics. Keywords: Hepatitis C, antiviral, nucleoside, ProTide, monophosphates Cite this Article Elsharif NA, Dakeel O. Review Article about Modified Nucleosides "(ProTide)" as Potential Anti-HCV Therapeutics. Research and Reviews: A Journal of Pharmaceutical Science. 2017; 8(1): 32–39p.
Development and Validation of a New Stability-Indicating HPLC Method for the Determination of Rosiglitazone in Tablets
Rosiglitazone (ROS) is an antidiabetic drug belonging to the thiazolidine class. A new stability-indicating high-performance chromatographic (HPLC) method was developed for the determination of ROS in pharmaceuticals, and validated for its suitability following the ICH guidelines. Chromatography was performed on a Chromatopack (250×4.6 mm; 5 µm particle size) column using phosphate buffer of pH 3.2 and methanol (70:30 v/v) as mobile phase pumped at a flow rate of 1 ml min-1 with UV-detection at 220 nm. The influences of mobile phase composition, buffer pH, flow rate and column temperature on the retention behaviour of the analyte were carefully studied and optimized. Quantification was based on peak area measurement and mean peak area-concentration plot was linear (r = 0.9999) over 7–525 µg mL-1 concentration range. Robustness of the method was assessed by performing the analysis under slightly altered chromatographic conditions; whereas ruggedness was determined with analysis being done by different analysts using different columns. The method was found to be selective as shown by results of placebo and synthetic mixture analyses. The method was applied to the determination of ROS in tablets and the results agreed well with the label claim and those obtained by a reference method. As part of degradation study, ROS was subjected to forced degradation under acid, base, oxidant, heat and light-induced stress conditions, and the results indicated that the drug was susceptible to base and oxidant-induced stress conditions and inert to other stress conditions. Keywords: Rosiglitazone, determination, HPLC, pharmaceuticals, stability-indicating Cite this Article Basavaiah K, Rajendraprasad N. Development and Validation of a New Stability-Indicating HPLC Method for the Determination of Rosiglitazone in Tablets. Research and Reviews: A Journal of Pharmaceutical Science. 2017; 8(1): 1–9p.
Current Updates on Risk Factors of Hepatocellular Carcinoma
Hepatocellular carcinoma (HCC) has a rising incidence in India frequently due to high prevalence of viral hepatitis, alcoholism, aflatoxin and its complications. HCC may affect more than 100 out of 100,000 people who live in some parts of Asia and Africa. Whatever that affects your probability of getting an ailment is called risk factor. Several risk factors, such as sex and place where you were born, are out of your control but other risk factors depend on your choices. This article summarizes the well-known risk factors of HCC such as alcoholism, viral hepatitis (hepatitis B infection is more common in Asia and hepatitis C is more common in the United States), aflatoxin in stapled foods, nonalcoholic steatohepatitis, diabetes & obesity, hemochromatosis, alpha-1-antitrypsin deficiency; and minor risk factors such as anabolic steroids, vinyl chloride, arsenic, parasitic infection, smoking and dietary sugar. Keywords: Hepatocellular carcinoma, aflatoxin, viral hepatitis, alcoholism Cite this Article Usmani A, Mishra A. Current Updates on Risk Factors of Hepatocellular Carcinoma. Research and Reviews: A Journal of Pharmaceutical Science. 2017; 8(1): 23–31p.
High-Performance Liquid Chromatographic Assay of Nateglinide and its Stability Study
Nateglinide (NTG) is a D-phenylalanine derivative used in the treatment of type-2 diabetes mellitus. An accurate, sensitive and reproducible high-performance liquid chromatographic (HPLC) method has been developed and validated for the quantification of NTG in pharmaceutical samples. The drug was eluted from Inertsil ODS 3V (150×4.6 mm; 5 µm particle size) column at 30ᴼC with a mobile phase consisting of phosphate buffer of pH 3.3 and methanol (70:30 v/v). The flow rate was 1 mlmin-1 and the UV detector was set at 210 nm to monitor the effluent. The retention behaviour of NTG as a function of mobile phase pH, composition and flowrate was investigated. Quantification was achieved by the measurement of mean peak area and the calibration curve was linear (r=0.9998) over the concentration range, 1–300 µg.ml-1. Limits of detection (LOD) and quantification (LOQ), calculated as per ICH guidelines, were 0.1 and 0.3 µg.ml-1, respectively. Intra-day and inter-day precisions expressed as RSD were <1% and the corresponding accuracies were better than 1.2% (RE). The method was also validated for robustness, ruggedness and selectivity. The method was applied to the determination of NTG in commercial tablets and the results agreed well with the label claim and those obtained by the reference method. Accuracy was also assessed by recovery test via standard-addition procedure. As part of degradation study, drug was subjected to forced degradation via acid- and base- hydrolysis, oxidation, thermolysis and photolysis, and the results revealed that the drug was degraded completely under oxidative stress condition and partly under base-induced stress condition. The drug remained intact when subjected to other stress conditions. Keywords: Nateglinide, determination, HPLC, pharmaceuticals, stress-testing Cite this Article Basavaiah K, Rajendraprasad N, Vinay KB. High-Performance Liquid Chromatographic Assay of Nateglinide and its Stability Study. Research and Reviews: A Journal of Pharmaceutical Science. 2016; 7(3): 41–52p.
Factors Affecting Implementation of Pharmaceutical Care at Jimma University Specialized Hospital, South West Ethiopia
Pharmaceutical care is the responsible provision of medicine therapy for the purpose of a definite outcome that improves a patient’s quality of life. It is a necessary element of healthcare and the concept implies the active participation of the patient in medicine therapy decisions and, the cooperation of healthcare providers across disciplines. This study was conducted to explore factors that affect the implementation of pharmaceutical care at Jimma University Specialized Hospital (JUSH). A prospective cross-sectional study with semi-structured self-administered questionnaire was conducted and complete survey technique was used for pharmacists working at JUSH and pharmacy post-graduate students. Fifty nine questionnaires were retrieved from the respondents that make the response rate around 89.39%. Significantly more than half of the respondents (69.49%) were male and slightly more than half (55.93%) were able enough to communicate through both Amharic and Afan Oromo. Lack of space and inappropriate layout within the pharmacy was found to be the strongest challenging factor for pharmaceutical care implementation at JUSH with 50.85 and 33.89% strongly agree and agree, respectively. Even though, the feasibility of pharmaceutical care in Ethiopia health system has been assured in previous studies, it is not well implemented at JUSH yet and is found in its early stage. Lack of space, trained personnel and time were identified in this study as inhibiting factors and therefore, enough and appropriate space and, sufficient pharmacists should be employed and freed to a greater extent from performing routine tasks which could be delegated with supervision to train supportive personnel, thereby expanding professional pharmacy service. Keywords: Pharmaceutical care, Implementation, Barrier, Jimma University Specialized Hospital Cite this Article Gebremichael Tesfay, Shibiru Tesema, Eliyas Kadi Abafita. Factors Affecting Implementation of Pharmaceutical Care at Jimma University Specialized Hospital, South West Ethiopia, Research and Reviews: A Journal of Pharmaceutical Science. 2016; 7(3): 30–40p.
Alcoholic and Aqueous Extract of Eucaluyptus Globules Posses Antimicrobial Activity and Antifungal Property Confined only to Alcoholic Extract
Alcoholic and aqueous extract of leaves of Eucalyptus globulus was studied for in vitro for its antimicrobial and antifungal activity. The study was done against gram-positive bacteria (Staphylococcus aureus), gram-negative bacteria (Escherichia coil and Pseudomonas aeruginosa) and fungus (Candida albicans). The evaluation was done by determining its inhibition zone. Result demonstrated that alcoholic extract has broad spectrum antibacterial and antifungal activity on gram-positive bacteria, gram-negative bacteria and fungus, whereas the aqueous extract has only broad spectrum antibacterial activity. Our study confirms the antibacterial and antifungal property of E. globules. Keywords: Eucalyptus globules, anti bacterial, amoxicillin, ciprofloxacin Cite this Article Pushpaveni C, Rekha S, Iswar Hazarika et al. Alcoholic and Aqueous Extract of Eucaluyptus Globules Posses Antimicrobial Activity and Antifungal Property Confined only to Alcoholic Extract. Research and Reviews: A Journal of Pharmaceutical Science. 2016; 7(3): 26–29p.
Colloidosomes: An Inherent Rigid Vesicle with Controlled Drug Distribution
Colloidosomes are hollow capsules whose shell is composed of closely packed uniform colloidal particles. To date, colloidosomes have been fabricated using colloidal assembly at liquid-liquid interfaces. This system also solves the problem of insolubility, instability, rapid degradation and widely used in specialized areas like protein delivery, gene delivery, targeting to brain, tumour targeting, etc. In the series of vascular systems, colloidosome is the advanced tool in drug delivery. Colloidosomes have a great, encapsulation efficacy with a wide control over size, permeability, mechanical strength and compatibility. Moreover, the release of larger encapsulated materials from such traditional colloidosomes relies on external triggers such as, changes in osmotic pressure or mechanical forces to crushor break open the capsule; this precludes precise control of the release response. These limitations highlight the need for a flexible technique to fabricate colloidosomes that enables both, control of the permeability to small species and a high degree of sensitivity to a release trigger. The types, properties, fabrication techniques, characterization and recent works on colloidosomes are compiled in this work. Keywords: Colloidosomes, core materials, emulsion droplets, fused colloidal particles, microcapsules Cite this Article Chavda Vivek P, Soniwala Moinuddin M, Chavda Jayant R. Colloidosomes: An Inherent Rigid Vesicle with Controlled Drug Distribution. Research and Reviews: A Journal of Pharmaceutical Science. 2016; 7(3): 12–25p.
Titrimetric and Spectrophotometric Assay of Diethylcarbamazine Citrate in Pharmaceuticals using Permanganate as Oxidant
Two titrimetric and one spectrophotometric methods are described for the determination of diethylcarbamazine citrate in bulk drug and dosage forms using permanganate as an oxidimetric agent. In method A, the drug solution in H2SO4 is titrated directly at 800C to a pink end point. DEC was treated with a measured excess of standard permanganate in H2SO4 medium, and after a contact time of 5 min, the residual oxidant back titrated with ammonium ferrous sulphate to a colorless end point (method B). Spectrophotometry is based on the measurement of the unreacted permanganate at 550 nm after the reaction between DEC and permanganate in H2SO4 medium is ensured to be complete (method C). In all methods, the amount of permanganate reacted was related to the amount/concentration of DEC. Experimental variables associated with the assay were carefully examined and optimized for better performance characteristics. Both the titrimetric methods are applicableover 1–10 mg range and the reaction follows 1:3 and 1:4 (DEC:KMnO4) stoichiometry in direct and indirect methods, respectively. In spectrophotometry, Beer's law is obeyed in the inverse manner, and linearity is observed in the range 2.5–30 µg ml-1 with a molar absorptivity value of 8.03×103 l mol-1 cm-1. The limits of detection (LOD) and quantification (LOQ) were calculated to be 0.12 and 0.35 µg ml-1, respectively. The methods were validated for precision and accuracy, robustness and ruggedness and selectivity. The methods were applied to the determination of DEC in tablets and suspension with satisfactory results. The accuracy of the methods was also assessed by recovery study via standard-addition procedure. Keywords: Diethylcarbamazine citrate, assay, titrimetry, spectrophotometry, permanganate, pharmaceuticals Cite this Article Nagib Qarah AS, Basavaiah K. Titrimetric and Spectrophotometric Assay of Diethylcarbamazine Citrate in Pharmaceuticals using Permanganate as Oxidant. Research and Reviews: A Journal of Pharmaceutical Science. 2016; 7(3): 1–11p.
Pharmacognostical and Pharmaceutical Analysis of Amavatari Rasa- A Herbo-mineral Compound
Amavatari Rasa is a herbo-mineral formulation, composed of processed mercury, sulphar, Terminalia chebula Retz, Terminalia bellerica Roxb., Phyllanthus embilica (Embelica officinalis Gaertn), Plambagozeylenica Linn., Commiphora wightii (Arn) Bhand and Ricinuscommunis Linn. This formulation is routinely practiced in cases of Rheumatoid Arthritis, but preliminary physicochemical and pharmacognostical profiles are not available. Considering this, an attempt has been made to develop this profile. Pharmacognostical study of raw drugs was carried out. Organoleptic features of fine powder made out of crude drugs were within the standard range. Loss on drying (LOD) was 0.5% w/w, total ash14.5% w/w, acid insoluble ash3.5%w/w and pH 6.5 was obtained as a result of analytical studies. High Performance Thin Layer Chromatography (HPTLC) showed difference of results when the sample scanned at two wave lengths i.e., 254 nm and 366 nm having 14 and 12 spots respectively. This shows presence of certain constituents in the powder and is helpful for the easy separation of these constituents. All above parameters helps to prepare the finger printing of classical drug Amavatari Rasa. Keywords: Amavatari Rasa, Rheumatoid Arthritis, HPTLC, Pharmacognostical study, Amalaki Cite this Article Sonam S. Bhinde, P.K. Prajapati, Galib, Harisha C.R, VJ Shukla. Pharmacognostical and Pharmaceutical Analysis of Amavatari Rasa- A Herbo-mineral Compound. Research and Reviews: A Journal of Pharmaceutical Science. 2016; 7(2): 6–10p.
Novel Synthesis of Encapsulated Super Paramagnetic Iron Nanoparticles (Fe3O4) and its Evaluation in Drug Delivery System
Nanoparticles can be defined as solid, submicron, colloidal particles ranging in size from 10–100 nm in diameter, generally but not necessarily made of natural or synthetic polymers, in which drugs can be adsorbed, entrapped, that exhibit new or enhanced size-dependent properties as compared to microparticles. Iron oxide nanoparticles are often magnetic by nature, which means that they obey Coulomb’s law, and can be manipulated by an external magnetic field gradient. Magnetic drug delivery system works on the delivery of magnetic nanoparticles (MNPs) loaded with drug to the tumor site under the influence of external magnetic field. MNPs because of their high magnetic responsiveness, biodegradability, high delivery efficiency and potential targeting function is a possible material as drug delivery system, since drug-loaded MNPs can be directly injected into solid tumors and are expected to be held in place by an external magnetic field and release of drug in controlled manner. In the present research study, synthesis, characterization and in vitro rate studies of super paramagnetic iron nanoparticles coated with oleic acid (OA) has been carried out. The nanoparticles synthesized in the present study had an average particle size of ~30 nm. Poly(lactic-co-glycolic acid) (PLGA)-based polymeric nanocarrier encapsulated with the drug, i.e., β-Caryophyllene and MNPs as anticancer drug delivery was constructed. This efficiently reduces tumor growth thus providing a concept for the utilization of present formulation in sesquiterpene-based anticancer therapies. Evaluation of β-Caryophyllene loaded MNPs was successfully carried out and correlation coefficient (R2) value and drug released was found to be 0.999 and 97%, respectively for 48 h at pH 7.0. The entrapment efficiency and drug loading of β-Caryophyllene-MNPs in the PLGA-based nanoparticles was found to be high. Keywords: Iron oxide nanoparticles, anticancer, β-Caryophyllene, less toxic chemicals Cite this Article Swathi D, Devi S, Nikitha. Novel Synthesis of Encapsulated Super Paramagnetic Iron Nanoparticles (Fe3O4) and its Evaluation in Drug Delivery System. Research and Reviews: A Journal of Pharmaceutical Science. 2016; 7(2): 11–24p.
Physico-Chemical, Phyto-Chemical and HPTLC Analysis of Root of Melia azedarach Linn
Mahanimba, botanically known as Melia azedarach L. is an important medicinal plant of Ayurveda. Different parts of Mahanimba are widely used to treat many ailments. Its root is used in Gridhrasi (sciatica) and also used as an ingredient of many Ayurvedic formulations. Present study was carried out to evaluate physicochemical, phyto-chemical and HPTLC analysis of root of M. azedarach Linn. following standard guidelines. Results of physicochemical study revealed that, root powder has loss on drying 3.71% w/w, total ash content 9.45% w/w, water soluble extractive 15.56% w/w, alcohol soluble extractive 6.00% w/w, and pH (5% aqua solution v/w) 5.5. Tannins, steroid, glycosides were important phyto-constituents of root extract. HPTLC study showed six spots at 254 nm i.e. 0.05, 0.12, 0.25, 0.68, 0.83 and 0.93; and five spots in 366 nm i.e. 0.05, 0.12, 0.20, 0.77 and 0.83. The observations made in this study may help to develop the standards of qualitative and quantitative parameters with regard to identification, quality and purity of Melia azedarach root. Keywords: Mahanimba, Melia azedarach, physicochemical, phyto-chemical, HPTLC study Cite this Article Vekariya Shweta R, Krushnkumar Taviad, Nishteswar Kara et al. Physico-Chemical, Phyto-Chemical and HPTLC Analysis of Root of Melia azedarach Linn. Research and Reviews: A Journal of Pharmaceutical Science. 2016; 7(2): 1–5p.
Advances in Wound Healing Products and Procedures: A Review
Victorious wound care involves optimizing patient’s local and systemic conditions in combination with an ideal wound healing environment. Numerous products have been developed till date to influence this wound environment and to provide a pathogen-free, protected, and an area free from moisture for healing to occur in acceleration. Many novel products are being introduced to replace or augment various substrates in the wound healing cascade. With the abundance of available products, the goal is to find the most appropriate modality or combination of modalities to optimize healing. This review looks at the most modern applications of silver in microbial prophylaxis and treatment, including issues involving resistance and side effects, the latest uses of negative pressure wound devices, advanced dressings and skin substitutes, biologic wound products including growth factor applications, and hyperbaric oxygen as an adjunct in wound healing. Keywords: Wound healing, silver, negative pressure wound devices, hyperbaric oxygen, skin substitutes Cite this Article Iswar Hazarika, Anju Das, Vineeth Chandy. Advances in Wound Healing Products and Procedures: A Review. Research & Reviews: A Journal of Pharmaceutical Science. 2016; 7(2): 40–51p.
Enhancement of Bioavailability of Clopidogrel Using Different Solubility Enhancement Techniques
Bioavailability is the key determinant of a drug for its therapeutic effectiveness, which in turn depends upon the solubility of that drug in gastro intestinal fluid. Clopidogrel is a BCS class II drug. Drugs of this category have low solubility and high permeability, so their bioavailability is less. This can be overcome by doing pharmaceutic modifications on it. In the present study, three different modifications, namely, complexation, solvent deposition and surface solid dispersion were utilized to improve the solubility. Preformulation studies included solubility, melting point determination and compatibility studies. FTIR, solubility analysis, in vitro drug release study and kinetic studies were done for all the formulations. Solubility study results showed better solubility of formulations. The mechanism of drug release from formulations was found to be super case 2 transport. From all these evaluations, the F3Sol.D was taken as better formulation. The F3Sol.D was subjected to further evaluation before formulating it into capsule form. The values of angle of repose and Carrs index show that the powder is having good flow properties. F3Sol.D was formulated into capsule. Capsules were evaluated for properties like content uniformity, weight uniformity and disintegration. In vitro dissolution studies showed 96% release at 60th min. Clopidogrel capsules were found to pass one month stability studies as per ICH guidelines. Keywords: Clopidogrel, solubility enhancement techniques, encapsulation complex, solvent deposition, surface solid dispersion Cite this Article Arun Raj R, Nadiya KK, Jyoti Harindran. Enhancement of Bioavailability of Clopidogrel Using Different Solubility Enhancement Techniques. Research and Reviews: A Journal of Pharmaceutical Science. 2016; 7(2): 25–39p.
Formulation and Evaluation of Verapamil Solid Dispersion Tablets for Solubility Enhancement
This study was mainly designed to solve the drawbacks of conventional verapamil solid dosage form, low bioavailability and limited clinical efficacy, by preparing solid dispersion. Verapamil solid dispersion was developed by kneading method, melt solvent method and co-precipitation method to modify the release and enhance solubility of the drug. The physical state of the dispersed verapamil in the polymer matrix was characterized by differential scanning calorimetry, powder X-ray diffraction, scanning electron microscopy, Fourier-transform infrared spectroscopy, super saturation solubility testing and dissolution studies. Verapamil solid dispersions (FT 9) were formulated into tablets by direct compression method. On comparing with pure drug and physical mixture, the dissolution of verapamil solid dispersion was enhanced dramatically. Formulation FT 9 showed faster drug release in comparison to other formulations and marketed tablet. Formulation FT 9 follows first order kinetics and the release mechanism is super case II transport mechanism. The results of accelerated stability study indicated that there was no significant change in the tablets. The present study conclusively indicated that the use of various solid dispersion methods by using water soluble carriers improved the solubility of poorly water soluble drug. Keywords: Solid dispersion, Verapamil, tablets, solubility enhancement Cite this Article Arun Raj R, Das Anju C, Sreerekha S, et al. Formulation and Evaluation of Verapamil Solid Dispersion Tablets for Solubility Enhancement. Research and Reviews: A Journal of Pharmaceutical Science. 2016; 7(1): 39–54p.
Design, Synthesis and Evaluation of Antitubercular Activity of Mannich Bases of Isoniazid-Containing Thiazolidin-4-one Rings
Isoniazid (INH), the established antitubercular drug was selected as the lead for the design and development of antitubercular agents by many researchers. 4-thiazolidinones are well known heterocyclic compounds for their spectrum of biological activities such as antibacterial, antifungal [1], anticancer [2], antitubercular, anthelmintic, anti-inflammatory [3], analgesic [4], antithyroid, local anaesthetic, monoamine oxidase inhibition, anti-Toxoplasma gondii activity etc [5]. Modification of thiazolidinones via Mannich reaction to improve biological activity is also reported [6]. A series of novel Mannich bases were designed from 4-thiazolidinones of INH using in silico studies. Docking studies were performed at Mtb enoyl acp reductase (4DRE) which is the binding site of INH. The derivatives exhibiting best docking scores were prepared from 2, 3-disubstituted-4-thiazolidinones by treating with formaldehyde and various secondary amines. 2, 3-disubstituted-4-thiazolidinones in turn were obtained from a series of INH Schiff bases by reaction with thioglycolic acid. Structures of the newly synthesized compounds were assigned on the basis of elemental analysis, IR, 1H NMR, 13CNMR and mass spectral studies. The newly synthesized compounds were screened for their in vitro antitubercular activity using Alamar blue assay method and the hepatotoxicity was determined by MTT assay using Chang liver cells. MB1V-4—the Mannich base of N-[2-(4-chlorophenyl)-4-oxo-1, 3-thiazolidin-3-yl] pyridine-4-carboxamide with nitrotriazolone (NTO)—exhibited the best antitubercular activity (sensitive at 1.6 µg/ml); in comparison with the standard parent drug INH (sensitive at 3.12 µg/ml). The percentage viability produced by MB1V-4 for in vitro hepatotoxicity screening was better than the percentage viability produced by INH itself. Keywords: Isoniazid (INH), 4-thiazolidinone, Mannich base, Nitrotriazolone (NTO), Alamar blue, Chang liver cell, in vitro hepatotoxicity Cite this Article Thomas B, Harindran J. Design, Synthesis and Evaluation of Antitubercular Activity of Mannich Bases of Isoniazid-Containing Thiazolidin-4-one Rings. Research and Reviews: A Journal of Pharmaceutical Science. 2016; 7(1): 1–12p.
Active versus Passive Microbiological Air Sampling Risk Assessment: Relation and Comparative Study in Pharmaceutical Industry
Microbiological environmental monitoring of pharmaceutical manufacturing area is an essential task for control of the quality during medicinal dosage forms production. However, thorough scientific approach is critical to elucidate the full potential of microbiological test results and its significance. In the present study, 205 passive and 451 active air samples were withdrawn during course of ten months from air in class C production facility, dedicated for manufacturing of liquid and semisolid pharmaceuticals. Microbial counts of samples were enumerated and recorded then the results were trended and analyzed using commercial statistical software package. The outcome of data analysis showed that the general trend lines were shifted towards increasing of bioburden. For convenience, data were grouped into three main categories viz. passive air samples (PAS), active air samples (AAS) of manufacturing rooms and AAS for the main corridor and airlocks (AAScal). PAS bioburden counts were significantly lower than both AAS and AAScal which were not appreciably different from each other. However, they showed significant correlation between each other. Interestingly, there was significant linear relationship between AAS and both of PAS and AAScal which have pooled slope equals 0.72. Risk of failure for microbiological samples was higher for AAScal than AAS and AAS than PAS. The former was expected due to nature of the activity and the later because of the difference in the sensitivity. The currently applied analysis provided insight for quality monitoring and evaluation of bioburden in air of clean rooms in addition to rapid spotting of defects for immediate corrections. Keywords: Environmental monitoring, pharmaceutical manufacturing, passive air, active air, out-of-control Cite this Article Eissa ME, Mahmoud AM, Nouby AS. Active vs. Passive Microbiological Air Sampling Risk Assessment: Relation and Comparative Study in Pharmaceutical Industry. Research and Reviews: A Journal of Pharmaceutical Science. 2016; 7(1): 13–27p.
Comparison Study of the Reactivity of 2-Acetyl Heterocyclic Compound toward Aldol Condensation with Benzaldehyde Derivatives
Some new chalcones have been synthesized by condensation of 2-acetyl pyrrol, 3-acetyl pyridine and 3-acetyl indole with various aromatic aldehydes in 25% alcoholic alkali. The synthesized compounds were identified by spectral and physical methods. From the time of reactions and the yield of the products, we can state that there were some obvious differences in the reactivity between the heterocyclic compounds used. Keywords: Reactivity, chalcone, aldol condensation, heterocyclic compounds, benzaldehyde Cite this Article Khlafulla Abdulrahim M, Al Mohamad F. Comparison Study of the Reactivity of 2-Acetyl Heterocyclic Compound toward Aldol Condensation with Benzaldehyde Derivatives. Research and Reviews: A Journal of Pharmaceutical Science. 2016; 7(1): 34–38p.
HPTLC: An Important Tool for Estimation of Phytoconstituents
Abstract HPTLC (High-performance thin layer chromatography) technique is widely employed in pharmaceutical industry for the process development, identification and estimation of adulterants in herbal formulations and helps in estimation and identification of pesticide content, mycotoxins and in quality control of nutraceuticals. For the herbal extracts and especially for the botanical drugs, the issue of stability is of exceptional importance. Standardization is required for the development of an accurate biological activity and for maintaining the quality of an herbal formulation. HPTLC is a simple technique and has many advantages over TLC as it is more sensitive techniques which can run more samples in a shorter period of time. The material needed and the methodology used in handling the machine is described in detail. The quality assurance of herbal formulation is an initial step for the herbal drug industry and other drug development organization for meeting the quality standards. It is mainly employed in estimation of the compounds with low or moderate polarities and particular suitable tool for stability testing for herbal medicinal products and for identification of the phytoconstituents available in herbs. Keywords: HPTLC, Phytoconstituents, Stability, Biological activity, Herbal formulations Cite this Article Neeraj Choudhary, HPTLC: An Important Tool for Estimation of Phytoconstituents, Research and Reviews: A Journal of Pharmaceutical Science. 2016; 7(1): 28–33p.