Formulation, characterization, evaluation and in vitro study of transfersomal gel medroxyprogesterone acetate for transdermal drug delivery

Iskandarsyah, Camelia Dwi Putri Masrijal, Harmita

Research output: Contribution to journalArticlepeer-review

Abstract

A hormonal contraception progestin such as medroxyprogesterone acetate (MPA) is used to helps regulate ovulation thus as a part of contraception hormone therapy as a method of birth control. This study aimed to formulate, characterized, evaluated transfersomal gel containing medroxyprogesterone acetate and to increased subcutaneous penetration of medroxyprogesterone acetate. In this research, three transfersomes formulas were prepared and optimized, e.g. F1, F2 and F3 with phosphatidylcholine: tween 80 concentration were 90:10; 85:15; and 75:25, respectively. F2 was the best formula with the highest entrapment efficiency 81.20±0.42 %, Average 81.35 ±0.78 nm, morphology of vesicles were spheres, indeks polidispersity 0.198±0.012 and zeta potential was-34.83±0.64 mV. The transpersonal gel (FGT) containing F2, and non-transpersonal gel containing MPA in methanol(FG) were prepared. In vitro penetration test were conducted to both of them using Franz Diffusion cells. Analysis of medroxyprogesterone acetate used a high performance liquid chromatographic (HPLC) method with an ultraviolet detector on reversed-phase C18, 5µm; 150 x 4.6 mmcolumn; using acetonitrile-0.1% formic acid (60:40/v:v) and was detected at a wavelength of 240 nm with flow rate at 1.0 mL/min. Gel stability evaluation results showed that FGT was better than FG on pH stability, viscosity and rheological properties. Based on in vitro penetration study, cumulative subcutaneous penetration of medroxyprogesterone acetate from FGT was 2356.45 ± 197.73 ng.cm−2 and from FG 359.15 ± 13.60 ng.cm−2, respectively. Flux value for FGT and FG were 112.77 ± 6,47 ng.cm−2 .hr−1and 17.99 ± 4.81 ng.cm−2 .hr−1, respectively. It could be concluded that transfersomal gel medroxyprogesterone acetate for transdermal drug delivery increased cumulative transdermal penetration of medroxyprogesterone acetate by six times more than non-transfersomal gel dosage form.

Original languageEnglish
Pages (from-to)5373-5381
Number of pages9
JournalInternational Journal of Research in Pharmaceutical Sciences
Volume11
Issue number4
DOIs
Publication statusPublished - 7 Oct 2020

Keywords

  • Characterization
  • Formulation
  • Gel
  • In Vitro Study
  • Medroxyprogesterone Acetate
  • Transdermal
  • Transfersome

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