Development and Evaluation of Niosomal Gel for TransdermalApplication of steroidal API

Sharma Rupali,Sharma Shekhar,Sardana Satish,Diwan Anupama,Vyas Amisha

doi:10.47392/irjash.2020.84

Abstract

Niosomal drug delivery system serves as drug depots within the body that release the drug in a controlled manner through its bilayer, providing the enclosed drug to be released with sustainedaction.Transdermal drug delivery system for steroidal drug molecules through the development of a niosomal gel is needed for an optimized drug delivery system due to various problems associated with conventional treatment of steroidal molecule. The objective of this study was to develop a niosomalgel-based formulation system for testosterone steroidal molecule dissolved in a mixture of non-ionic surfactant and cholesterol in nanoparticulate form and evaluation of niosomal gel by different optimization parameters. The niosomal gel dispersion was prepared by heating system technique.The drug loaded niosomes showed much less vesicle size [10 - 500 nm] and good PDI, which means that the drug loaded can easily permeate the skin. Niosomal based gel was formulated by using the xanthan gum as gelling agent by optimizing different concentration of different gelling agents to get the best consistency of final niosomal gel. Various measurement parameters such as product quality, pH, purity, homogeneity, spread ability, viscosity, In vitro drug release, particle size determination, zeta potential, FTIR studies and TEM analysis were done to optimize the best batch.Entrapment efficiency was very good with value of 92.17 ± 0.02 percent. Niosomal gel has been found to exhibit strong consistency, good homogeneity, spread ability, and viscosity parameters.Studies of FTIR showed no excipient interaction with the API molecule. TEM images showed that all the particles were in uniform range in niosomal dispersion.Data on the release of in vitro drugs also showed that the release pattern was comparable to the industry formula. The niosomalbased gel formulation developed can be a promising alternative to delivering steroidalbased molecule to minimize the side effects due to skin problems as well as to increase the permeation rate of steroids by using transdermal drug delivery.

Highlights

Niosomes are non-ionic surfactants with multilamellar vesicles obtained on hydration of synthetic non-ionic surfactants, with or without incorporation of sterol such as cholesterol or other lipids
All the chemicals and cholesterol and surfactant were purchased from Sigma Aldrich and of analytical grade. 2.1 Pre- formulation Study: Pre-formulation studies was done to optimize the different physicochemical properties of API molecule as well as to design and formulate the niosomal dispersion and niosomal gel
[8] The reformulation studies were performed by U.V.spectroscopy,HPLCandExcipient compatibility with the drug by using FTIR. 3

Summary

Introduction

Niosomes are non-ionic surfactants with multilamellar vesicles obtained on hydration of synthetic non-ionic surfactants, with or without incorporation of sterol such as cholesterol or other lipids. Niosomes have been extensively studied for their potential to serve as a carrier for the delivery of drugs, hormones, antigens and other biologically active drugs. The presence of the steroidal system in the niosomes improves the rigidity of the bilayer, affect the bilayer fluidity and permeability andprotect the drug molecules from the degradation due to some unwanted biological effects. Targeted drug delivery can be achieved using niosomes the drug is delivered directly to the body part where the therapeutic effect is required. The therapeutic efficacy of the drugs isimproved by reducing the clearance rate, targeting to the specific site and by protecting the encapsulated drug. Drug targeting reduces the dose which leads to subsequent decrease in the side effects. The vesicular system in the niosomes make them capable off encapsulating hydrophilic and lipophilic substances. Hydrophilic drugs are usually encapsulated in the inner aqueous core or adsorbed on the bilayer surfaces, while lipophilic substances are entrapped by their partitioning into the lipophilic domain of the bilayers [Figure 1][3]

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Results