DEVELOPMENT AND EVALUATION OF TRANSDERMAL DRUG DELIVERY OF SALBUTAMOL SULPHATE VIA ETHOSOMESAbstract
Asthma is a chronic disease; there is a need for a drug delivery system that maintains adequate therapeutic concentrations for a longer duration of action to improve better clinical efficacy. Salbutamol sulphate (SS) is a widely prescribed drug to treat asthma though it has short plasma half-life and undergoes extensive first-pass metabolism. Thus, it necessitates frequent administration by oral route to maintain adequate plasma concentrations. Hence an attempt was made to formulate and evaluate transdermal ethosomal gel formulations of SS to improve therapeutic efficiency and to reduce the dosage regimen. Ethosomal suspensions of drugs were prepared using phosphatidylcholine, alcohol, propylene glycol, and cholesterol. Then, suspensions were used to develop gels by incorporating them into carbopol. Formulations were evaluated for vesicular size, size distribution, scanning electron microscopy, drug content estimation, drug entrapment efficiency, in-vitro diffusion studies, Z-Average, polydispersity index (PDI), and zeta potential measurement. Analytical studies confirmed the absence of drug and polymer interaction. Drug content of ethosomal suspensions and gel formulations was found uniform, and microscopic images displayed that vesicles are spherical shape. PDI values indicated a broad size distribution of ethosomes. Zeta potential values confirmed the dispersion stability of ethosomal vesicles in suspensions. The drug release rate from ethosomal gels extended up to 12 h, progressively increased with an increase in alcohol concentrations, and decreased with increased concentration of carbopol 934. The drug release rate followed zero-order and non-Fickian diffusion mechanism. The whole study disclosed that transdermal gel formulations of SS via ethosomes hold potential for providing controlled release by achieving adequate bioavailability and thus could enhance the overall life quality of asthmatic patients.
S. K. M. Lokamatha * and M. P. Ahmed
Department of Pharmaceutics, V. L. College of Pharmacy, Raichur, Karnataka, India.
23 September 2019
19 March 2020
23 August 2020
01 September 2020