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Ethosomal gel: a novel choice for topical delivery of the antipsychotic drug Ziprasidone Hydrochloride

Abstract

Oral delivery of antipsychotic drugs like Ziprasidone HCl has a disadvantage of gastric disturbance and lack of adherence to the treatment. In the present study, Ziprasidone HCl loaded ethosomal gel was formulated to avoid the disadvantages of oral delivery.

The ethosomes were prepared using Lipoid S 75 with Isopropyl alcohol and Propylene glycol as the solvents. The formulated ethosomes were evaluated for different parameters like particle size, poly dispersibility index and entrapment efficiency. Based on diffusion studies, optimized ethosomal formulation was incorporated in carbopol 934 gel base. The final dosage form of ethosomal gel was evaluated for physical characteristics, drug content and proceeded with ex- vivo skin permeation studies.

The maximum percentage of drug permeated after 24 hours was found to be 93.30±0.168. The flux was found to be 52.05± 0.564µg/hr/cm2. From the kinetic model fitting results, it was concluded that the ethosomal gel followed the first order kinetics and the higher “R2” values of the Korsmeyer Peppas model (R2=0.934, n=0.54) indicate that the encapsulating polymer is the responsible factor in controlling the release of the drug.

The ethosomal gel loaded with ziprasidone HCl improves the bioavailability of ziprasidone HCl as well as surpassing drawbacks with oral delivery.

Keywords:
Ethosomes; Ziprasidone HCl; Ethosomal Ggel; Lipoid S75; Carbopol 934

Universidade de São Paulo, Faculdade de Ciências Farmacêuticas Av. Prof. Lineu Prestes, n. 580, 05508-000 S. Paulo/SP Brasil, Tel.: (55 11) 3091-3824 - São Paulo - SP - Brazil
E-mail: bjps@usp.br