Dinesh Puri

Solid Lipid Nanoparticles Approach for Lymphatic Targeting Through Intraduodenal Delivery of Quetiapine Fumarate

BACKGROUND Lymphatic route is one of the prominent routes for improving the poor bioavailability of the drugs which undergo extensive hepatic first pass metabolism. Nanocarriers (solid lipid nanoparticles) offer a new drug delivery system that could hold great promise for attaining the bioavailability enhancement along with controlled and site specific drug delivery. OBJECTIVE The aim of the present research work was to prepare and optimized the Quetiapine fumarate (an antipsychotic drug) loaded solid lipid nanoparticles for lymphatic targeting through intraduodenal administration. METHOD Thirteen quetiapine fumarate loaded solid lipid nanoparticle formulations were developed using different lipids by Microemulsion technique and optimized by box behnken design. RESULTS Optimized formulation (Q9) had a mean particle size of 230.38 nm with 75.92% of entrapment efficiency. The percentage drug release after 24 h was found to be 95.81%. A significant difference (P<0.05) was found in the in vitro release data of optimized formulation as compared to marketed formulation. In vitro release data of optimized formulation (Q9) was subjected to zero order, first order and Higuchi model to evaluate the release kinetics. Higuchi model was found to be the best fitted model with highest value of correlation coefficient (R2= 0.999). In vivo studies for optimized solid lipid nanoparticles formulation and drug suspension were performed on male Wistar rats after intraduodenal administration and several pharmacokinetic parameters were determined. AUC (0-∞) of optimized formulation was significantly (P<0.01) more than that of drug suspension. Bioavailability of quetiapine in solid lipid nanoparticles was 2.76 fold increased after intraduodenal administration as compared with that of drug suspension. CONCLUSION On the basis of results of in vitro study, Q9 formulation was selected as optimized formulation. It exhibited better bioavailability as compared to drug suspension. It can be concluded that solid lipid nanoparticles are potential carrier for improving quetiapine bioavailability through lymphatic delivery.

Solid lipid nanoparticles for nose to brain delivery of donepezil: formulation, optimization by Box–Behnken design, in vitro and in vivo evaluation

Abstract This study was aimed at preparing and characterizing solid lipid nanoparticles (SLNs) of donepezil (DPL) for delivery to brain via nasal route. SLNs were prepared by solvent emulsification diffusion technique using glyceryl monostearate (GMS) as lipid and blend of tween 80 and poloxamer 188 (1:1) as surfactant. Box–Behnken design was applied for optimization by using drug to lipid ratio, surfactant concentration and stirring time as dependent variables and their effect were observed on particles size, entrapment efficiency and drug loading. Optimized formulation was evaluated for particle size, zeta potential, entrapment efficiency, drug loading, morphological analysis, crystallinity, in vitro drug release, in vivo (biodistribution, pharmacokinetic and Gama scintigraphy) studies. For optimized formulation (OD3), value of particle size, zeta potential, percent in vitro release, entrapment efficiency and drug loading was found to be 121.0 nm, –24.1 mV, 89.35%, 67.95% and 12.15%, respectively. Pharmacokinetic and biodistribution studies were performed on albino Wistar rats and value of AUC0–∞ in brain for DPL-SLNs i.n. was found to be nearly 2.61 times higher than that of DPL-Sol i.v., whereas 2.26 times superior than DPL-Sol administered intranasally. The scintigraphy images were taken in rabbit and result revealed the localization of drug in brain.

Formulation and evaluation of antihelminthic polyherbal tablets

From time immemorial, man has been depending on plants as medicine. Helminthes infections are among the most common infections in man, affecting a large proportion of the world’s population. These helminthic diseases can be treated by various herbal drugs. The purpose of the present work was to formulate antihelminthic tablets. In this work, a spray dried-powder was used, which was obtained from the extract of different part of seven plants that were used in helminthic disease. The different tablets were prepared by using different types of disintegrating agents and various excipients. All parameters related to physicochemical property, trace metal and microbial examination of the spray-dried powder showed that these were within limits and could be used for the tablet formulation. The granules of the spray-dried powder were prepared by a wet granulation technique using isopropyl alcohol. The blends were evaluated for flow properties and for compressibility, which were found to be good. The tablets were prepared using a single rotatory punching machine, in which the punch size was 11 mm×8 mm, and formulated caplet-type tablets. These tablets were evaluated for the colour, odor, thickness and diameter, with visual inspection for any defects, weight variation, hardness, friability and in vitro disintegration time. Key words: Antihelminthic, herbal tablets, spray-dried powder

ANTIFUNGAL ACTIVITY OF AQUEOUS AND HYDROALCOHOLIC EXTRACTS OF DESERT PLANT DHAMASA AND THEIR COMPARISON BY STATISTICAL ANALYSIS

Herbal plant Dhamasa is widely distributed in deserts and dry areas of India, Pakistan to tropical Africa. Botanical name of Dhamasa is Fagonia schweinfurthii Hadidi (Family-Zygophyllaceae). Traditionally it is boiled in water and its bath is taken for allergies and other skin diseases. In this study the antifungal activity of the aqueous and hydroalcoholic extracts of Dhamasa were evaluated. Aqueous extract was prepared by decoction method and hydroalcoholic extract was prepared by soxhletion method. The evaluation of antifungal activity of plant extracts was determined as the minimum inhibitory concentration (MIC) followed by cup plate method against three fungal strains. Inherent antifungal activity of aqueous as well as hydro-alcoholic extract of Dhamasa was found. For the comparison of results Student’s t test was applied on the values of diameters of zones of inhibitions produced by aqueous and hydroalcoholic extracts. The result indicated that aqueous as fungal strains. Statistical analysis of results reveal that there was no significant difference in the antifungal potential of aqueous as well as hydroalcoholic extract possess almost equal antifungal potential against selected. These extract can be used in various antifungal topical preparations.

DEVELOPMENT AND VALIDATION OF UV SPECTROSCOPIC METHOD FOR THE ESTIMATION OF AQUEOUS EXTRACT OF FAGONIA SCHWEINFURTHII HADIDI

A simple, rapid, accurate, precise, and economic spectrophotometric method for aqueous extract of Fagonia schweinfurthii hadidi have been developed. Aqueous extract of plant was obtained from decoction process of coarse powder of whole plant. Aqueous extract of plant shows absorbance maximum at 265 nm when Phosphate Buffer of pH 6.8 and 0.1N HCl used as solvent system . Calibration curves were constructed in phosphate buffer pH 6.8 and 0.1 N HCl. Beer’s law was obeyed in the concentration range of 25 - 350 µg/ml. In phosphate buffer pH 6.8 the equations and R 2 obtained , were y = 0.0025x - 0.0083 and R 2 = 0.9995 respectively and i n 0.1N HCl t he equations and R 2 obtained w ere y = 0.0024x + 0.0181 and R 2 = 0.9987 respectively. Validation of developed