FORMULATION AND EVALUATION OF BESIFLOXACIN NON-ERODIBLE OCULAR INSERTS

Objective: Ocular inserts offer many advantages over conventional dosage forms, like increased ocular residence, the possibility of releasing a drug at a slow and constant rate, accurate dosing, exclusion of preservatives, and increased shelf life. Besifloxacin is a very important drug for the treatment of infectious conjunctivitis. The present study was aimed to formulate and evaluate Besifloxacin Non-Erodible Ocular Insert using Pullulan and polyvinyl pyrrolidone as a drug reservoir, PEG 400 as a plasticizer, and Eudragit RS-100 as a rate-controlling membrane. Methods: Central composite design was employed to study the effect of independent variables, i.e., effects of Pullulan amount (X1) and PVP (X2) on the dependent variables, i.e., % moisture absorption and In vitro diffusion rate. After evaluation of all thirteen batches of ocular insert reservoir formulation, BSF2 and BSF4 were selected as a satisfactory formulation and was sandwiched between rate-controlling membrane, which was made up of Eudragit RS-100 (3 and 5%). Results: The drug content of all formulations was found to be in the range of 95.33 to 99.89 %. In vitro diffusion of Besifloxacin from reservoir formulations (BSF1 to BSF13) was found to be 62.44 to 70.62 %. In vitro diffusion rate of an ocular insert of Besifloxacin can offer benefits such as increasing residence time, prolonging drug release in the eye for 24 h. Eudragit RS-100, as a sustained drug release polymer, showed promising sustained released action. Conclusion: The study concluded that Besifloxacin non-erodible ocular inserts can be successfully developed using Pullulan and polyvinyl pyrrolidone, which will sustain the release of the drug also reduce the frequency of administration, and thereby may help to improve patient compliance.

FORMULATION AND EVALUATION OF ANTIFUNGAL CREAM OF CHLORPHENESIN

Objective: The main aim of our research was to develop an Antifungal cream formulation consisting of Chlorphenesin for the treatment of Fungal infections. Topical route is the most suitable route for skin infections. Methods: The development of topical drug delivery systems designed to have systemic effects appears to be beneficial for a number of drugs on account of several advantages over conventional dosage forms(or) routes of drug administration. An Antifungal cream formulation consisting of Chlorphenesin was prepared. Results: The formulation was subjected to in vitro diffusion studies. Microbiological studies were performed to find out the safety of materials used in the formulation. Conclusion: The developed cream consisting of Cholrphnesin was found to be safe and effective for the treatment of fungal infection.

Methanolic Extraction, Formulation and Evaluation of Herbal Transdermal Patches of Azadirachta indica A. Juss

At present, synthetic drugs form a major line of treatment in the management of many diseases and currently available as transdermal patches. Traditional medicine system is centuries old practice and again gaining importance. Hence, herbal products can be used to treat many diseases as transdermal patches. Neem leaves has antibacterial properties and can be used for controlling air borne bacterial contamination. Azadirachta Indica. A. Juss (neem) very useful traditional plant. The present study was carried out to extract, formulate and evaluate a transdermal patches containing Azadirachta indica A. Juss The total four Transdermal patches were prepared by solvent casting method and evaluated for physicochemical characteristics such as weight variation, thickness, drug content uniformity, folding endurance, In-vitro diffusion, ex-vivo permeation studies and anti-Bacterial screening test. The infrared spectroscopy showed that there was no incompatibility between drug and polymer. The In-vitro diffusion studies of Transdermal patches of Neem showed percentage of drug release from 65.2% to 92.06% at the end of 21hrs. The ex-vivo permeation study was carried out for optimized formulation (M2) using goat abdomen skin as barrier and showed percentage drug release 89.6% at the end of 21hrs. Release kinetics data showed that all the formulations followed zero order kinetics with non-Fickian diffusion mechanism. The anti-bacterial screening study showed good anti-bacterial activity against Bascillus subtilis and Pseudomonas aeruginosa and zone of Inhibition (ZOI) was compared against standard antibiotic drugs i.e. Penicillin and Streptomycin.

FORMULATION, DEVELOPMENT AND EVALUATION OF TOPICAL INTRADERMAL DRUG DELIVERY SYSTEM FOR ANTI-ACNE PRODUCT

The objective of the present study was to explore the anti-acne activity of herbal drug extracts of curcumin by making complexes with varying concentrations of soya lecithin using the phase inversion technique. The preformulation studies were performed and indicated that using the resultant formulation FIM4 shows the maximum potency outcomes. The characterization and evaluation were carried using Fourier Transform Infrared Spectroscopy (FTIR) and using various parameters such as appearance, texture, pH determination, viscosity, spreadability, stability, drug content, saponification value, irritation, antibacterial activity and in vitro diffusion. From the study, it was concluded that the optimized formulation FIM4 show the best resulting potency with antimicrobial properties.

Design and development of zolmitriptan niosomal in situ nasal gel for the treatment of migrain

The objective of the present study was to development of Zolmitriptan (ZMT) niosomal in situ nasal gel formulation for migraine treatment. By intranasal route delivered drug to the central nervous system (CNS) through the olfactory lobes, which bypasses the first-pass metabolism and consequently enhances the bioavailability. Noisome of ZMT were prepared by using the lipid film hydration method. Optimized niosomal formulation was used to prepare in situ gel. The developed Noisomal formulations were characterized for vesicle size, shape, zeta potential, entrapment efficiency, drug content and in-vitro diffusion study, mucoadhesive strength, permeation study, FTIR, DSC and XRD studies. The FTIR and DSC studies predicted that there was no any interaction in drug and excipients. ZMT niosomes were showed particle size, Polydispersity index (PDI), Zeta potential, % entrapment efficiency and drug content, 149nm, 0.223, -28.9, 88.16±0.8 % and 96.23±1.2% respectively. In-vitro diffusion study of niosomes shows 96.23±0.7% at 8h. The permeation rate of in situ niosomes gel and the pure drug was about 98.56% and 79.46%, respectively. XRD & DSC studies were showed that reduce crystalinity in the formulations. The SEM images of niosomes were found spherical in shape to some extent showing particle size distribution. Thus, it can be concluded that developed ZMT niosomal in situ gel formulation can be considered as a promising system for which may reduce dose requirement, improve patient acceptability and efficient targeting drug delivery to the brain through the olfactory lobe for migraine treatment.

In Vitro Drug Release, Permeability, and Structural Test of Ciprofloxacin-Loaded Nanofibers

Nanofibers of the poorly water-soluble antibiotic ciprofloxacin (CIP) were fabricated in the form of an amorphous solid dispersion by using poly(vinyl pyrrolidone) as a polymer matrix, by the low-cost electrospinning method. The solubility of the nanofibers as well as their in vitro diffusion were remarkably higher than those of the CIP powder or the physical mixture of the two components. The fiber size and morphology were optimized, and it was found that the addition of the CIP to the electrospinning solution decreased the nanofiber diameter, leading to an increased specific surface area. Structural characterization confirmed the interactions between the drug and the polymer and the amorphous state of CIP inside the nanofibers. Since the solubility of CIP is pH-dependent, the in vitro solubility and dissolution studies were executed at different pH levels. The nanofiber sample with the finest morphology demonstrated a significant increase in solubility both in water and pH 7.4 buffer. Single medium and two-stage biorelevant dissolution studies were performed, and the release mechanism was described by mathematical models. Besides, in vitro diffusion from pH 6.8 to pH 7.4 notably increased when compared with the pure drug and physical mixture. Ciprofloxacin-loaded poly(vinyl pyrrolidone) (PVP) nanofibers can be considered as fast-dissolving formulations with improved physicochemical properties.

DESIGN AND CHARACTERIZATION OF NANOSPRAY WITH SELF-NANOEMULSIFYING DRUG DELIVERY SYSTEM USING SINERGISTIC COMBINATION OF MELASTOMA MALABATHRICUM L. FRACTION AND GENTAMICIN

Objective: This study aimed to design a formula using Design-Expert software to obtain optimal Self-Nanoemulsifying Drug Delivery System (SNEDDS) formulas and to analyze nanospray characteristics of optimal SNEDDS. Methods: The study began with preparing ethanol extract from Melastoma malabathricum. The extract was then fractionated using ethyl acetate. The formulation design stage began with a solubility test of Melastoma malabathricum fraction and gentamicin (MFG) in various surfactants, co-surfactants and oils. Furthermore, the 14 formula of SNEDDS with various compositions of the selected surfactants, co-surfactants and oils were formulated and evaluated with pH response and emulsification time. Analysis was carried out using Design-Expert software with the simplex lattice design method in order to obtain the optimal formula profile. The pH, emulsification time, particle size, and zeta potential of the nanospray from SNEDDS optimal formulas were physically characterized. Stability of SNEDDS and the nanospray was then tested with freeze-thaw cycling and in vitro diffusion studies with Franz diffusion. Results: Based on the study, the ratios of optimal formula SNEDDS composition of Tween 80, propylene glycol, and soybean oil were 2.69: 2.64: 1.67 parts. Nanospray with SNEDDS technology had characteristics of pH 5.61±0.16, emulsification time 7.68±0.18, particle size 270.7 nm, and zeta potential-37.20 mV, and it was stable. Conclusion: Nanospray can be formulated from optimal SNEDDS using Design-Expert software. Nanospray with SNEDDS technology has physical characteristics and is stable. In vitro diffusion studies revealed that the release of Melastoma malabathricum from nanospray was faster than that without preparation.

Evaluation of antipsoriatic activity of gel containing Pongamia pinnata extract on Imiquimod-induced psoriasis

Background Pongamia pinnata (Fabaceae) is among those categories of plants mentioned in Ayurveda and traditionally known to use in several types of disease and disorders. The objective of the present work was to investigate the anti-psoriatic activity of Pongamia pinnata leaves extracts in Herbal gel formulation. Results Hydroalcoholic leaves extract of Pongamia pinnata was first subjected to phytochemical screening and quantification of phytoconstituents. Herbal gel was prepared containing Pongamia pinnata extracts using Carbopol 934 as gelling agent. The prepared gel formulations were studied for pH, viscosity, Spreadability and in vitro diffusion studies. The imiquimod-induced psoriatic mouse model, showed a prominent anti-psoriatic activity of the extract as evident through index grading. Treatment with extract confirmed a noteworthy reduction in psoriasis in the treated groups as there was a considerable diminution in the thickness and scaling of skin. Conclusions Lack of proper treatment and disadvantages associated with allopathic medicines pave the way to extensive research in natural products with anti-psoriatic activity. The present research scientifically justified the anti-psoriatic activity of the Hydroalcoholic extracts of Pongamia pinnata leaves.