IN VITRO STUDY OF A TRANSFERSOMAL GEL PREPARATION CONTAINING LYNESTRENOL AS A TRANSDERMAL DRUG DELIVERY SYSTEM

Nurfitriyana Nurfitriyana,Iskandarsyah Iskandarsyah,Harmita Harmita

doi:10.22159/ijap.2020.v12s1.ff052

Nurfitriyana Nurfitriyana, Iskandarsyah Iskandarsyah + Show 1 more

Open Access

https://doi.org/10.22159/ijap.2020.v12s1.ff052

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Abstract

Objective: Lynestrenol, a progestin hormone derivative, can suppress the productions of endogenous estrogen and progesterone hormones (ovaries)to prevent ovulation. In this study, lynestrenol was included in various transfersomal gel preparations for its transdermal delivery into fat (F)-andnon-fat (NF)-containing skin tissues.Methods: Lynestrenol transfersome vesicles were prepared by encapsulating the drug in varied concentrations of phosphatidylcholine and Tween80 using lipid film hydration method. Transfersomes were produced in the form of gel preparations at a dose of 0.15 mg/week and evaluated fortheir particle size, percentage of entrapment efficiency, and particle polydispersity. We performed in vitro evaluations of the formulation variants F0(lynestrenol gel control) and F1 and F2 (lynestrenol transfersome gels) with variations in their phosphatidylcholine and Tween 80 content. We thenperformed an in vitro evaluation using the Franz diffusion cell (FDC) method for 12 h using all three formulations on F and NF-containing rat skin.Results: The FDC results demonstrated that lynestrenol was deposited into fat tissue and increased concentrations of Tween 80 (edge activator)increased lynestrenol delivery into this tissue. In addition, the percentages of drug penetration from NF rat skin treated with F0, F1, and F2 gels were19.56%, 20.13%, and 20.56%, respectively, and those from F rat skin were 17.16%, 17.38%, and 17.50%, respectively.Conclusion: In vitro evaluation using the FDC method indicates that transdermal drug delivery through to fat tissues using transfersomes is apromising method for lynestrenol delivery.

Highlights

Oral contraceptive tablets have been used for more than 50 years, but user self-discipline is required as they must be consumed regularly at the same times each day [1]
Materials Lynestrenol was purchased from IPC (Pirumadara, India); Tween 80 and Phospholipon® 90G (Soya phosphatidylcholine ≥91%) were purchased from lipoid GmbH (Ludwigshafen, Germany); potassium dihydrogen phosphate monohydrate, sodium hydroxide, and dichloromethane were purchased from Merck (Darmstadt, Germany); methylparaben, propylparaben, glycerine, and propylene glycol were purchased from Dow Chemical (Jakarta, Indonesia); and hydroxypropyl methylcellulose (HPMC) K4M, sodium metabisulfite, aquadest, and ethanol (96%) were purchased from Merck (Darmstadt, Germany)
The transfersomes prepared with a small concentration of the surfactant Tween 80 (F1) have a smaller size compared with those prepared using a higher concentration (F2)

Summary

Introduction

Oral contraceptive tablets have been used for more than 50 years, but user self-discipline is required as they must be consumed regularly at the same times each day [1]. Transdermal drug delivery systems have a number of advantages over oral pills, as they provide continuous administration of drug through the skin, which maintains constant plasma drug levels and avoids the peaks and troughs that are seen with oral drug administration [2]. The use of a transdermal system for contraception presents a number of clinical advantages over the conventional oral method. The drug is delivered directly into the systemic circulation, which avoids hepatic first-pass metabolism and maintains constant circulating drug concentrations [5]

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