An Overview : Natural Bio-enhancer’s in Formulation Development

Bioenhancers are chemical entities that are obtained from synthetic as well as natural sources. They are mainly used in formulation development to enhance the bioavailability of poorly solubilized drug molecule. The ideal characteristic of bioenhancers includes inertness, nontoxic, cost effective and decrease the dose of active constituents. There are lots of natural bioenhancers available such as piperine quercetin niaziridin, genistein, glycrrhyzin, curcumin. The review focus on plant based bioenhancers and their active principle that produces those effects. There is a need of extensive study on natural bioenhancers which can be utilized in formulation development. Keywords: bioenhancer, bioavailability, piperine, curcumi

Formulation and Evaluation of Fixed Dose Combination Tablets of Antifungal Drugs for Candida albicans Resistant to Fluconazole

Background: The emergence of Candida albicans strains resistant to fluconazole (FLZ) had raised interest on combining other antifungals with FLZ. In vitro and clinical studies had indicated synergistic interaction between terbinafine and FLZ against strains resistant to FLZ and improved therapeutic efficacy. Objective: Formulation and evaluation of fixed dose combination (FDC) tablets of terbinafine HCl (TH) and FLZ for avoidance of resistance and improved therapeutic efficacy against C. albicans infections.  Method: The compatibility of TH and FLZ together and with excipients was determined by FTIR spectroscopy. A UV-visible spectroscopic Q-absorbance ratio method was developed and validated for linearity, accuracy, precision, LOD and LOQ for simultaneous estimation of TH and FLZ. The FDC tablets was prepared by wet granulation using hydroxy propyl cellulose (1%, 2%, 3%, 4% and 5%) as binder and evaluated for pre-compression and post-compression parameters. Result and Discussion: The TH and FLZ were compatible together and with excipients used in FDC. The linearity range was found to be 0.5-3.0 µg/ml and 80-400 µg/ml for TH and FLZ, respectively. Percent RSD was less than 2% indicating good accuracy and precision for proposed method. The hardness and disintegration time of tablets increased and friability decreased with increased binder concentration. Formulation F2 and F3 showed more than 80% drug release within 30 minutes. Conclusion: The TH and FLZ were compatible and can be formulated as a FDC tablet. The UV-Visible spectrophotometric method developed for simultaneous estimation was simple, accurate and sensitive. Keywords: Terbinafine, Fluconazole, Q-absorbance, Fixed Dose Combination, Candida albican

Cubosomes: A Novel Carrier for Transdermal Drug Delivery

Cubosomes are square and rounded particles with internal cubic lattice. Cubosomes are thermodynamically stable and consist of honeycombed (cavernous) structures separating two internal aqueous channels and a large interfacial area. Cubosomes are nanoparticles which are self assembled liquid crystalline particles of certain surfactants with proper ratio of water with microstructure that provides unique properties of practical interest. Bicontinuous cubic liquid crystalline phase is optically clear and very viscous material has the unique structure at nanometer scale. The word bicontinuous refers to the division of the two continuous but non-intersecting aqueous regions by lipid bilayer that is twisted into space filling structure. Hydrating a surfactant or polar lipid that forms cubic phase and then dispersing a solid like phase into smaller particles usually forms a cubosomes. Self-assembled cubosomes as active drug delivery systems are receiving more and more attention and interest after the first discovery and nomination. They exhibit different internal cubic structure and composition with different drug-loading modalities. It has high internal surface area and cubic crystalline structures, relatively simple preparation method, biodegradability of lipids, the ability of encapsulating hydrophobic, hydrophilic and amphiphilic substances, targeting and controlled release of bioactive agents. Cubosomes are having wide range of applications in various fields and they can be characterized by various evaluation parameters. So, Cubosomes are gaining more attention in pharmaceutical field. Keywords: Cubosomes, Liquid crystal, drug-loading, hydrophilic, hydrophobic, amphiphilic

Method Development and Validation for Multicomponent Analysis of Rosuvastatin Calcium and Losartan Potassium in Bulk Drug by RP-HPLC

A simple, sensitive and specific liquid chromatographic method was developed for the simultaneous estimation of Rosuvastatin calcium and Losartan potassium in bulk form. Chromatographic conditions included the  Column C-18 (Shim-pack) 250 x 4.6 mm, particle size 5 µm , mobile phase acetonitrile,  methanol and water pH 3 (orthophosphoric acid) in the ratio 20:25:55 recorded  at 233 nm. The retention time were found to be   3.55 and 4.64 min and average percentage recovery 99.42% and 99.63% for Rosuvastatin calcium and Losartan potassium respectively. The proposed method was found to comply with ICH guidelines. Keyword: Rosuvastatin calcium, Losartan potassium, RP-HPLC, accuracy and linearity

Method development and validation for simultaneous estimation of methotrexate and curcumin in Bulk Drug by using RP-HPLC

Curcumin is the natural herb that shows effect in the treatment of cancer and rheumatoid arthritis and methotrexate is well known anticancer and anti-rheumatoid drug. Literature survey reveals that there was no method available for the selected drug combination. So, here an attempt has been made to develop simple, rapid and economic method for simultaneous estimation of methotrexate and curcumin in bulk drug by using RP-HPLC method. The percentage assay from optimized method was found to be 99.68% and 99.76% for methotrexate and curcumin respectively.  The proposed method was validated for  linearity, accuracy, precision and robustness according to ICH guidelines and were found to be   within the standard range. Keywords: RP- HPLC, methotrexate, Linearity, anticance

Formulation and Evaluation of Microsponges Gel of Havan Ash for the Treatment of Acne

The aim of this study was to develop the Microsponges containing Havan ash composed gel formulation for the treatment of Acne. Therefore, the topical formulation containing microsponges of Havan Ash will be formulated and evaluated. The preliminary investigation was carried out for the formulation of Havan ash loaded Microsponges by using quasi emulsion solvent diffusion method (MSF1-MSF6). In the preformulation studies of Havan ash the physical description and organoleptic properties, pH, acid insoluble ash, water-soluble ash, IR spectroscopy, identification test, rheological study, atomic absorption spectroscopy is also carried out. On the basis of particle size analysis of Microsponges, percentage yield formulation MSF5 containing Microsponges formula was selected for composition of topical gel formulation. Thus the different gel base formulation (G1-G3) using Carbopol-934 (1,1.5,2.0%) was prepared by emulsification method. By considering all the relevant, physicochemical parameters, G2 gel base was selected for further loading of Havan ash containing Microsponges. The MSF5 formulation was loaded into the selected gel base G2 (1.5%). Then the formulation and evaluation of Havan ash microsponges loaded gel was done. The formulation F3 has better results than other 4 formulations. F3 have its appearance silver colour, consistency very good, Grittiness –ve, homogeneity good, wash ability very good, pH 6.3, Spreadabilty (g.cm/sec) 14.4 ± 0.77 7and viscosity (cps) 18251 ± 50.12, have good result of psychometric analysis. With the revealed results by different evaluation parameters, it is concluded that microsponges drug delivery system has become highly competitive and rapidly evolving technology and more research are carrying out to optimize cost-effectiveness and efficacy of the therapy. Keywords: Havan ash, Antimicrobial, Microsponges, Acne vulgaris, Topical gel

Method Development and Validation for Multicomponent Analysis of Emtricitabine and Ritonavir in Bulk Drug by RP-HPLC

A simple, sensitive, economic and specific reverse phase liquid chromatographic method was developed for the simultaneous estimation of Emtricitabine and Ritonavir in bulk drug. Chromatographic conditions consisted of   C-18 Column (Shim-pack) 250 x 4.6 mm, particle size 5 µm , mobile phase combination of methanol and water (80:20), flow rate 1ml per minutes, run time 15 minutes and UV detection at 251nm. . The retention time for Emtricitabine and Ritonavir were found to be   3.25 and 7.8 min and average percentage recoveries 99.42% and 99.63% respectively. The validation parameters were found to comply with ICH guidelines. These methods can be further employed in future for the routine determination of Emtricitabine and Ritonavir in bulk drug and formulation. Keyword: Emtricitabine, Ritonavir, RP-HPLC, accuracy and linearity