Abstract

FORMULATION, OPTIMIZATION, AND CHARACTERIZATION OF GELS LOADED ETHOSOMAL VESICLES OF IMATINIB MESYLATE FOR MELANOMA

K. Uma Mageshwari*, K. Balakumar, Keerthana Devi M., Arjunan Karuppaiah, Anamika P.K.

ABSTRACT

The present study aimed to develop and characterize a vesicular ethosomal drug carrier system of Imatinib mesylate for Melanoma skin cancer. A three-level two factorial design was utilized to prepare nine batches of Imatinib Mesylate loaded ethosomes by a cold method using the ultrasonication technique by varying the composition of the drug, ethanol, and soya phosphatidylcholine. Ethosome formulations were characterized for compatibility, Vesicle size, % Drug content, % Entrapment efficiency, Surface morphology, invitro drug release, and stability studies. All nine batches of ethosomes were found to be below 500 nm with the least particle size of 54.19±1.92 nm for formulation EF 4. The entrapment efficiency was low and varied between 35.33±3.49% to 58.37±2.47% due to the hydrophilic nature of the drug. In vitro release studies in pH 7.4 phosphate buffer showed a maximum release of around 83 % in 24 hours. Considering parameters like size and entrapment efficiency, formulation EF7 (20% ethanol and 200 mg soyaphosphatidyl choline) with a particle size of 71.20±1.96 nm and 58.37±2.47% of the drug in nanoparticles was optimized for ethosomal gel with 1 %carbopol. The ethosomal-loaded different gels were studied using a Texture Analyzer. Carbopol gel-loaded ethosmes were found to have better drug content with good texture properties like firmness, spreadability, less stickiness, and elasticity than poloxamer gel. Hence, 1% (w/w) carbopol gel loaded with ethosomes containing 10 mg Imatinib Mesylate (also 20% ethanol, 200 mg phosphatidylcholine, and 2 ml propylene glycol) was found to be the optimized formulation for further studies.

Keywords: Ethosomes, Ethosomal gel, Melanoma, Imatinib Mesylate.