Nonionic surfactant based vesicles which are uni/multilamellar in structures are called niosomes. These vesicles contains an aqueous interior surrounded by one or more amphiphilic bilayer membrane forming surfactant which separates them from the bulk solution, and are also called as supramolecular aggregates. Niosomes, being an efficient drug delivery system, investigations are carried out to utilize this system to treat various disorders, to promote improved patient compliance, lesser side effects, reduction in dose, lesser dosage frequency, and higher amount of the drug at the particular site so as to lessen an excessive contact with the whole body. The Pharmacokinetic and Pharmacodynamic profile of Niosomal drug delivery system vary for various entrapped drugs. Drugs that are successful in the mitigation or treatment of CNS disorders should cross the BBB to reach the brain, as BBB seems to be an obstacle for a large number of drugs, including CNS active drugs. This article compiles recent techniques for the preparation and characterization of niosomes, the effect of formulation variables on its physicochemical properties and discussed about its effective applications in drug delivery.Critical packing parameter can be determined by the self-assembly of surfactants to vesicles. CPP=V/IcaHydrophobic tail volume (V), Hydrocarbon tail area (Ic), and Hydrophilic head group area (a) is also shown in fig. 2. I In nt te er rn na at ti io on na al l J Jo ou ur rn na al l o of f A Ap pp pl li ie ed d P Ph ha ar rm ma ac ce eu ut ti ic cs s
Objective: The present work was to formulate oral herbal tablets of Emblica officinalis extract and also with pure gallic acid, further to determine the dosage frequency through pharmacokinetic profiles obtained for the same. Methods:The Emblica officinalis fruits were suitably extracted and the concentration of gallic acid in Emblica officinalis extract was estimated by HPTLC (High-Performance Thin Layer Chromatography) with a comparison to pure form. Tablets were prepared with extract and synthetic form through direct compression technique by varying the process and formulation parameters. The formulated tablets were administered to rabbit models and their pharmacokinetic profile was studied after withdrawing blood samples through HPLC (High-Performance Liquid Chromatography). Results:The concentration of gallic acid in Emblica officinalis was found to be 8.21%. The pre and post compression parameters evaluated for the formulated batches found to be within the pharmacopoeial limits. The in vivo pharmacokinetic studies conducted in rabbit models showed that there were no significant differences with p-value between the pharmacokinetic data obtained for pure and extract gallic acid tablets. The Cmax was found to be 4.59±0.95 µg/ml in the extract form which was little low when compared to the pure form of 6.38±1.08 µg/ml. The t1/2 in the extract form was 6.0±0.33 h, whereas it was 4.92±0.36 h in the pure form of gallic acid. Conclusion:The Emblica officinalis extract tablet showed average t1/2 of 6 h, so about every 6 h one tablet compared to 4 h of t1/2 for pure gallic acid tablet can be the dosing frequency for the rabbit.
Objective: Aim of the study is to develop rivastigmine-loaded niosomal in situ gel via the intranasal route to the brain by crossing the Blood-Brain Barrier. For the treatment of Alzheimer’s disease, it provides a speedy onset of action, a faster therapeutic effect, avoidance of the first-pass metabolism, and enhanced bioavailability. Methods: Rivastigmine niosomal in situ nasal gel was developed, refined and tested with the goal of delivering the medicine to the brain via the intranasal route Rivastigmine niosomes were formulated by thin-film hydration technique, optimized using (32) factorial design and characterized for its physicochemical parameters. Rivastigmine-loaded niosomes were further incorporated into Carbopal-934P and HPMC-K4M liquid gelling system to form in situ nasal gel. The resulting solution was evaluated for several parameters including, viscosity at pH 5 and pH 6, gelling capacity and gelling time. Results: Optimized best formulation containing span 60 (A) and cholesterol (B) with (1:0.5) ratio identified from the model developed from Design-Expert®12 software, exhibited Entrapment efficiency (76.5±0.23%), particle size (933.4±0.14 nm), in vitro drug release maximum (68.94±0.26%) at 8th hour and further studied for its characteristics by SEM and TEM showed stable vesicles. Polynomial equations of Y1, Y2, and Y3 were conducted and ANOVA results showed a significant impact (p<0.05) on three levels. In vivo perfusion studies using rat model showed, the niosomes developed has good perfusion compared to pure drug with 27.2% of drug absorption in the brain at the end of 3 h. In vitro permeation of Rivastigmine through the dialysis membrane showed that 60.74% w/w drug permeated after 8 h. The formation of stable vesicles was proved by Zeta potential measurements and SEM analysis. Conclusion: Optimized formulation had greater perfusion and was expected to have a good bioavailability compared to conventional other drug delivery systems.
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