COMPARATIVE EVALUATION OF SELECTED POLYMERS AND PLASTICIZER ON TRANSDERMAL DRUG DELIVERY SYSTEM

Objective: The present work was aimed at preparation of transdermal patches by a solvent casting method using a varying concentration of polymers i.e. methocel (K15 and K100), ethocel (4 and 10), gelatin, chitosan, eudragit (RL and RS) grade using plasticizer (glycerin and propylene glycol).Methods: The ratio of drug to polymers and plasticizer was varied and the effect of formulation variables was studied. Prepared transdermal patches were evaluated for physicochemical properties, in-vitro permeation studies, content uniformity, primary skin irritation studies and FT-IR studies.Results: The formulated transdermal patch by using Methocel K 100 M showed good physical properties. The average weight of patches prepared using glycerin as a plasticizer were ranged from 42.33-67.00 mg and propylene glycol as a plasticizer were ranged from 40.67-67.67 mg. The percentage moisture absorption varies from 1.76 to 10.73 for patches formulated using glycerin and 2.28 to 7.97 for propylene glycol patches. The percentage moisture loss from patches prepared using glycerin was ranged from 2.75 to 11.54 and 2.87 to 12.02 from propylene glycol. The water vapour transmission rate from patches prepared using glycerin was ranged from 0.25 to 0.92 and 0.41 to 1.76. The formulated patch showed the acceptable quantity of medicament ranged from (100.20-101.05%). This result met the test content uniformity as per BP (85% to 115%). According to that, the drug was consistent throughout the patches. The formulation PGD is considered as the best formulation, since it shows a maximum in vitro drug release as 43.75 % at 24 h. The drug release kinetics studied showed that the majority of formulations was following zero order.Conclusion: In conclusion, controlled release transdermal drug delivery system patches of aliskiren can be prepared using polymer combinations, with a different plasticizer. The release rate of drug depends upon the polymer. However, release kinetics followed zero order

COMPARISON OF EFFECT OF PENETRATION ENHANCER ON DIFFERENT POLYMERS FOR DRUG DELIVERY

Objective: Aliskiren hemifumarate is used for the treatment of hypertension. The aim of this research to study the effect on the delivery of drug using natural and synthetic permeation enhancers like limonene, cineol, β-cyclodextrin, and oleic acid by using different polymers. As different penetration acts differently with polymers.Methods: Transdermal patches were prepared by the solvent evaporation technique. The controlled release polymers were used for the preparation of patches. The patches were prepared with different polymers and different plasticizer. The drug and polymer interaction study was performed by Fourier transform infrared spectra. In vitro permeation studies were conducted using pretreated cellophane membrane using franz diffusion cell. Results: The prepared patches were evaluated for in vitro drug release, and the release profile was varied from 52.32% PGH (oleic acid) to 87.63% B (cineol). The permeability coefficient was found in the range of 5.82 to 8.32 cm/h, and corresponding flux was found between 281.61 to 729.08 µg/cm2/h on the prepared patches and statistical analysis performed using t-test (p<0.005).Conclusion: On the basis of the obtained results, it was concluded that patch prepared using methocel k 15 m as a polymer, glycerin as plasticizer and cineol as a permeation enhancer shows the maximum release. The increase in the release due to increase in the flux

Preformulation screening of lipids using solubility parameter concept in conjunction with experimental research to develop ceftriaxone loaded nanostructured lipid carriers

Development of ceftriaxone loaded nanostructured lipid carriers to increase permeability of ceftriaxone across uninflamed meninges after parenteral administration. Lipids were selected by theoretical and experimental techniques and optimization of NLCs done by response surface methodology using Box-Behnken design. The Δδt for glyceryl monostearate and Capryol90 were 4.39 and 2.92 respectively. The drug had maximum solubility of 0.175% (w/w) in glycerol monostearate and 2.56g of Capryol90 dissolved 10mg of drug. The binary mixture consisted of glyceryl monostearate and Capryol90 in a ratio of 70:30. The optimized NLCs particle size was 130.54nm, polydispersity index 0.28, % entrapment efficiency 44.32%, zeta potential -29.05mV, and % drug loading 8.10%. In vitro permeability of ceftriaxone loaded NLCs was 5.06x10-6 cm/s; evidently, the NLCs pervaded through uninflamed meninges, which, was further confirmed from in vivo biodistribution studies. The ratio of drug concentration between brain and plasma for ceftriaxone loaded NLCs was 0.29 and that for ceftriaxone solution was 0.02. With 44.32% entrapment of the drug in NLCs the biodistribution of ceftriaxone was enhanced 7.9 times compared with that of ceftriaxone solution. DSC and XRD studies revealed formation of imperfect crystalline NLCs. NLCs improved permeability of ceftriaxone through uninflamed meninges resulting in better management of CNS infections

FORMULATION, OPTIMIZATION AND CHARACTERIZATION OF ZIPRASIDONE NANOCRYSTALS PREPARED BY MEDIA MILLING TECHNIQUE

Objective: Today, nanotechnology has a variety of application areas. Pharmacy is one of the most important application fields of nanotechnology. Preparation of nano-particular drug-delivery system, such as nano-crystals improve the solubility and bio-availability of poorly water soluble drugs.Methods: Ziprasidone (ZIP) is a low water soluble drug (Bio-pharmaceutical classification system) and is used as a lipid regulating agent. In this study, a rapid and simple media milling method was used for the preparation of ziprasidone (ZIP) Nanocrystals. The use of sonication after media milling process reduced the milling time significantly. Different concentrations of stabilizers (Kollidone and Tween 80) were tested in the preparation of ZIP nanocrystals. The finest ZIP nanocrystals were obtained by 4 g ZIP, 4 g kollidone and 4 g Tween 80.Results: The size and zeta potential of the finest ZIP nanocrystals were 238.2±2.5 nm and-19.6±0.1 mv, respectively. The morphology of dried ZIP nanocrystals was observed using scanning electron microscopy. Differential scanning calorimetry of ZIP and ZIP nanocrystals confirmed that there was no interaction between ZIP and stabilizers. Compared with ZIP, the solubility of ZIP nanocrystals increased significantly.Conclusion: Media milling technology was successfully used for the formulation of poor water soluble drugs. Nano-sized drug particles prepared by media milling technique could improve the solubility and bio-availability of those drugs.Â

EFFECT OF ZEIN ON CIPROFLOXACIN FLOATING TABLETS

Objective: This work was aimed to formulate and evaluate the effect of zein on Ciprofloxacin HCl floating tablets. According to previous studies, it was set up to be useful against bacteria i.e. Helicobacter pylori which leads to peptic ulcers. Thus, it is quite necessary to enhance the Gastric Retention Time for similar medicines. Methods: 12 different floating tablets of Ciprofloxacin HCl were formulated with wet granulation method with a rise in the concentration of zein. Further, all different formulations prepared were evaluated for different parameters i.e. pre-compression considerations, along with post-compression factors like weight variation, content uniformity, thickness, visual assessment, hardness, friability, buoyancy studies i.e. total floating time as well as floating lag time, swelling index, dissolution and drug release kinetics. Results: The F6 formulation was considered to be among finest formulation with appropriate hardness. It was found that with the increasing concentration of zein, the hardness of tablets was also increased. It showed TFT of more than 7 h, FLT of 310 sec, a swelling index time of 99.5 % in 4 hr, while drug release kinetics was found to follow Higuchi Model. Conclusion: Overall it was also found that HPMCK-100M is more effective as compared to HPMC-K15M and Zein has a major role in increasing the hardness of tablets. In the future, the investigation will be continued with the following studies: An in vivo study and a long-term stability study

CURRENT MEASURES AGAINST OPHTHALMIC COMPLICATIONS OF DIABETES MELLITUS-A SHORT REVIEW

Diabetes mellitus (DM) is a metabolic disorder, whose prevalence is predicted to rise shortly. The present review focuses on the various ocular complications associated with DM, and the various ophthalmic formulation approaches developed to treat the same. Diabetic macular edema (DME), diabetic retinopathy, cataracts, and glaucoma are some of the major vision-threatening complications linked to DM. The ocular route of drug delivery has undergone several advancements in recent decades, the introduction of various novel drug delivery systems (DDS), various modifications in the existing formulation approaches, development of custom-designed personalized medications, being some of the major developments introduced in the field of ocular drug delivery. Due to the application of state-of-the-art technologies in the field of innovations related to ocular DDS, patients have been immensely benefited by the current modes of ocular treatment imparting fewer side effects, enhanced penetration, sustained drug effect, and so on. The present review includes and emphasizes the gradual development that has occurred from the conventional ophthalmic dosage forms to the currently reported novel ocular drug delivery approaches along with the related clinical research works

OBETICHOLIC ACID: AN INSIGHT INTO A QUANTITATIVE DETERMINATION AND METHODOLOGICAL VALIDATION THROUGH NUCLEAR MAGNETIC RESONANCE

Objective: The research work unveils the use of nuclear magnetic resonance (NMR) technique for quantitative determination and method validation of obeticholic acid. As standard expository methodology for more up to date medications or formulations may not be available in pharmacopeias, hence it is fundamental need to create novel analytical procedures which should be precise and accurate. Methods: Proton (1H) and carbon (13C) NMR analysis were initially performed to confirm the preliminary authenticity of obeticholic acid API. Method validation was accomplished on the basis of standard guidelines for the parameters, in which tetramethylbenzene as an internal standard and deuterated dimethyl sulfoxide as a diluent were used to assess the obeticholic acid. Results: For the quantification of the drug, the proton nuclear magnetic resonance signals at 0.602 ppm and 6.86 ppm corresponding to the analyte proton of drug and internal standard respectively were used. The curve equation calculated from the regression method, the relative-standard-deviation and correlation-coefficient were found to be 0.743% and 0.9989 respectively, indicating good linearity. Consequently, the quantitative assay of the drug was found to be 99.91% in linearity with limit of detection and quantification values as 0.0773 mg and 0.2344 mg respectively, making successful the study of method validation for obeticholic acid. Conclusion: The advantage of the method was that no reference standard of analyte drug was required for quantification and method validation. The method is non-destructive and can be applied for quantification of drug in commercial pharmaceutical formulation products

Statistical Optimization of Process Parameters Influencing Biotransformation of Plant Tannin into Gallic Acid under Solid–Liquid Fermentation

<p class="MsoNormal" style="text-align: justify; line-height: 200%;"><span style="color: black;">Gallic acid </span><span style="line-height: 200%; color: black;">(3, 4, 5-trihydroxy benzoic acid), an important organic acid for synthesis of </span><span style="color: black;">propyl gallate and trimethoprim, was produced by solid-liquid fermentation using <em>Rhizopus oryzae</em> NRRL 21498. Evolutionary operation (EVOP)-factorial design and response surface methodology was applied successfully to elucidate the effect of different process parameters influencing biotransformation of natural tannin (powdered chebulic myrobalan fruit) to gallic acid. At 28<sup>O</sup>C, 70% relative humidity, pH 6, 72h of fermentation period, 3ml inoculum volume and 25g substrate weight resulted maximum gallic acid yield of 93.29%.</span></p&gt