Current Issue : July - September Volume : 2013 Issue Number : 3 Articles : 10 Articles
The vesicular approach of drug delivery is mainly comprised of the colloidal particles formed as a concentric bio molecular layer that are capable of encapsulating drugs inside themselves. They are usually employed to deliver the associated drug through the q, into the deeper tissues and systemic circulation. These carriers are composed of the lipids similar to the lipids present in the stratum corneum. These Structures consist of either a stack of multi-bilayer or a large number of single lipid bilayer, in the form of closed vesicles. These vesicles are utilized as a useful model representing the biological membranes and act as a well-situated medium intended for the delivery of a variety of agents. Ethosomes are the advanced approach to vesicular delivery comprised of hydroalcoholic phospholipid in which the concentration of ethanol is relatively in the range of 20-50%. The synergistic effect of comparatively high concentration of ethanol in Ethosomes has been the main reason intended for their superior skin permeability by simultaneously getting squeezed and causing the disruption on lipid bilayers present in the stratum corneum. Various drugs when associated with an ethosomes appear to have much more efficient delivery systems than classic vesicular approaches. For example, Bacitracin, a polypeptide antibiotic, was delivered from ethosomes to a depth of 200 μm in a human cadaver skin, whereas its delivery of classic liposomes was negligible. Study with an ethosomal erythromycin demonstrated an improved antibacterial action, flux of Trihexyl phenidyl Hydrochloride an anti-Parkinsonian agent was substantially higher than that from conventional liposomes. Similar results have been reported for Propranolol Hydrochloride and Sodium Diclofenac. Ethosomal formulations of testosterone have been compared with marketed transdermal patches, shows significantly higher AUC and Cmax values....
The main objective of this article is to focus on advancement in niosomal technology and its applications. Niosomes are novel and targeted drug delivery carriers and are the area of major interest of modern pharmaceutical research. Various vesicular systems such as liposomes, niosomes, transferosomes, erythrosomes, pharmacosomes and ethosomes have been used to improve the drug delivery. Niosomes play an increasing important role in drug delivery to the target as they can reduce toxicity and modifying pharmacokinetic and bioavailability and improve therapeutic performance. Niosomes are non ionic surfactant vesicles, obtained by hydration of thin film formed from mixture of cholesterol and non ionic surfactants that reduce the toxicity problem associated with other vesicular systems. They are multilamellar and unilamellar vesicles based on the method of preparation. The aim of this article is to review recent trends undertaken to develop niosomes carrier and combination of the niosomal technology with the in situ gelling technology to provide control and sustained delivery of drugs....
Celiprolol hydrochloride (CLH) is a novel third generation drug used for the treatment of hypertension. It is a hydrophilic compound that is incompletely absorbed from gastrointestinal tract and leads to dose dependant low oral bioavailability. This study was aimed to determine CLH permeability through isolated rat skin by the use of iontophoresis approach. Glickfeld diffusion cell was used for in-vitro permeation study. Anodal iontophoretic delivery composition was optimized by evaluating pH of the vehicle solution, concentration of NaCl, current density, type of current and drug concentration. Increasing the pH of alkaline borate buffer from 8 to 10 resulted in doubling of the iontophoretic flux of CLH. Maximum drug permeation was found in presence of 0.1 M NaCl, more or less amount of NaCl was found to decrease drug permeation from alkaline borate buffer solution. The drug permeation was 46.125 µg/cm2/hr and 32.557 µg/cm2/hr in presence of pulsed depolarized DC current and continuous DC current, respectively. With increasing current density, the drug permeation was increasing almost linearly. Concentration of drug was observed non significant factor in alkaline borate buffer containing NaCl. Drug permeated from human cadaver skin (415.118±6.72 µg/cm2) was found to be laser than isolated rat skin (501.293±6.47 µg/cm2) when optimized composition was studied for comparative in-vitro permeation....
Aim-In this study Solid Lipid Nanoparticles (SLNs) containing 5-Fluorourasil, nonsteroidal antiestrogens have been loaded by high shear hot homogenization followed by ultrasonication technique and to be used as breast cancer therapy, was prepared to decrease the dose as well as to increase the bioavailability of drug. Methods-A 32 factorial design was utilized to optimize the formulation where the concentration of lipid stearic acid (X1) and concentration of surfactant lipoid (X2) were taken as independent variables. 5-Fluorourasil loaded SLNs seem to have dimensional properties useful for oral administration. SLN was characterized by Differential Scanning Calorimetery (DSC), morphology, in vitro drug release, Zeta Potential and Particle Size. Results-Preliminary study of anticancer activity in vitro, carried out on MCF-7 cell line (human breast cancer cells), demonstrated that SLNs, containing 5-Fluorourasil showed an antitumoral activity comparable to free drug. 5-Fluorourasil loaded SLNs seem to have dimensional properties useful for oral administration. Polynomial equations and response surface plots were generated for all dependent variables using multiple regression analysis. The results of characterization studies strongly support the potential application of 5-Fluorourasil-loaded SLNs as a carrier system. Conclusion-The SLN presented here are well suited for certain drug delivery applications, particularly breast cancer therapy....
Multiparticulate system is one of the most widely accepted technologies in the pharmaceutical industries. The present study aims to prepare controlled release multiparticulates of Zidovudine by Solution / suspension layering technique using two different release retardants (Eudragit RS-100 and Eudragit RL-100, and their combination) in three different release retardant concentrations (10%, 20%, 30%). This method involves the deposition of successive layers of solution and/or suspensions of drug substances and binders on starter seeds. In principle, the factors that control coating processes apply to solution or suspension layering. The prepared multiparticulates were evaluated for friability, drug content uniformity, micromeritic property, density and percentage yield. The release rate was evaluated by dissolution studies. FT-IR was done to establish drug polymer compatibility. Study concluded that solution and/or suspensions layering of Zidovudine can be effectively used for drug loading on non-pareil seeds. FT-IR study concluded that there is no interaction between Zidovudine, Eudragit RS-100 and Eudragit RL-100. It was also found that formulation having Eudragit RS-100 have more retarding capacity with drug than the Eudragit RL-100 in both formulations and shows promising result. From dissolution parameter of the prepared multiparticulates it is concluded that formulation A8 possesses the required characteristics of oral controlled release formulation....
The aim of the work was to improve the dissolution properties of the poorly soluble drug, Telmisartan by the liquisolid compaction technique. The study was carried out by applying full factorial design. Components of formulation such as amount of propylene glycol and ratio of carrier to coating material R were selected as independent variables and dissolution amount, hardness & disintegration time were taken as dependent variable. Liquid load factor (Lf) and excipients ratio were calculated with mathematical model to give the required amount of excipients necessary for preparing the tablets. Telmisartan liquisolid tablet formulations made, complied the different official and non-official tests. Significantly improved dissolution profile was observed for F7 as compared to that of marketed formulation as indicated by difference factor 51. The study demonstrated with confidence that the liquisolid technique is promising approach for improvement of solubility of poorly soluble drugs....
Nimesulide has extensively used for the treatment of acute pain, osteoarthritis and primary dysmenorrhoea in adolescents and adults above 12 years old and in the treatment of rheumatoid arthritis and inflammatory conditions. The purpose of the study was to investigate the nimesulide microemulsion based gel formulation for topical delivery. Five microemulsions were prepared using isopropyl myristate as oil phase, tween80/propylene glycol as surfactant/ co-surfactant and an aqueous solution as the external phase. Pseudo ternary phase diagrams were constructed to obtain the concentration range of oil, surfactant and co-surfactant for microemulsion formation. From these microemulsions gels were prepared and are evaluated for spreadability, viscosity, homogeneity, consistency, pH etc. In vitro drug release studies were conducted using excised rat skins. Carbopol 934 was used to prepare the micro emulsion based hydrogel for improving the viscosity of microemulsion for topical administration. The micro emulsion based hydrogel showed a good stability and human skin tolerability. These results indicate that the micro emulsion based hydrogel may be a promising vehicle for topical delivery of nimesulide....
The purpose of this study was to investigate microemulsion-based hydrogel (MBH) as a topical delivery system for acyclovir. Topical delivery of acyclovir in the forms of microemulsion, MBH and the commercial cream was evaluated in-vitro and in-vivo. The results of permeation test in-vivo in mice showed that compared with the commercial cream, MBH and microemulsion could significantly increase the permeation of acyclovir into both epidermis and dermis. Stability test showed that MBH stored at 4°C for 3 months had no significant change in physicochemical properties. Skin irritation test in rabbit demonstrated that single application or multiple applications of MBH did not cause any erythema or edema, slight skin irritation for microemulsion. Microstructure changes of skins after administration observed under light microscope and scanning electron microscope (SEM) might result from the interaction of the ingredients of microemulsion with skins, which was related with the permeation enhancement of acyclovir. It can be concluded that the MBH could be a promising vehicle for topical delivery of acyclovir....
Skin is the largest organ of the body and protects from physical, chemical and biological grievance. It acts as barrier for permeation especially for hydrophilic and ionic drugs due to the lipophilic nature of the stratum corneum. Iontophoresis offers transfer of the molecules from stratum corneum to the systemic circulation by the application of the tolerable electricity. Iontophoresis provides pulsatile delivery of drug and avoids first pass metabolism of drug. The present review covers advantages, disadvantages and criteria of the drug selection for iontophoresis. This review also focuses on the principle and mechanism of iontophoresis. Pathways for iontophoretic transfer and iontophoretic devices are also included in this review. This review gives idea about factors affecting iontophoresis and conjugation of iontophoresis with other techniques. Formulation method used for the iontophoresis and in-vitro iontophoresis study are also covered....
The present study deals with optimization and formulation design by using factorial design software (Design Expert 8.0.7.1, Statease, USA). Response surface plots and main effect plots were utilised to study effect of variables on the response parameters. Aspirin (ASP) loaded Solid lipid nanoparticles (NLCs) were prepared using optimised process parameters and by microemulsion method using melted Glyceryl monosterate (GMS) as an oil phase and Poloxomer 407 water solution as an aqueous phase. Formulated ASP-NLCs were characterised for particle size, polydispersity index, zeta potential, drug entrapment efficiency, in-vitro drug release, differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and for stability studies. Among all formulations NLC7 was found to be an optimized formulation on the basis of small particle size 54.50 nm, higher entrapment efficiency 93.04±0.22%, and higher in-vitro cumulative drug release 86.48%. DSC studies reveal that aspirin was stable in final formulation and compatibility with selected excipients in the formulation. Formulated NLCs loaded ASP nanoparticles can be deliver through oral, parenteral or topical routes for improvement of bioavailability and to avoid GI side effects of ASP....
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