FORMULATION DEVELOPMENT AND EVALUATION OF PRONIOSOMAL GEL OF ETHINYLESTRADIOL AND LEVONORGESTREL FOR ANTIFERTILITY TREATMENT

Shikha Baghel Chauhan; Tanveer Naved; Nayyar Parvez

doi:10.22159/ajpcr.2019.v12i1.29546

Authors

Shikha Baghel Chauhan Department of Pharmaceutics, Amity Institute of Pharmacy, Amity University, Noida, Uttar Pradesh, India.
Tanveer Naved Department of Pharmaceutics, Amity Institute of Pharmacy, Amity University, Noida, Uttar Pradesh, India.
Nayyar Parvez Department of Pharmacy, School of Medical and Allied Sciences, Galgotias University, Greater Noida, Uttar Pradesh, India.

DOI:

https://doi.org/10.22159/ajpcr.2019.v12i1.29546

Keywords:

Estradiol, Formulation development, Levonorgestrel, Transdermal matrix patches

Abstract

Objective: The purpose of this research was to develop and formulate proniosomal gel drug delivery system of ethinylestradiol and levonorgestrel for antifertility treatment that is capable of efficiently delivering entrapped drug over an extended period of time.

Methods: Ethinylestradiol and levonorgestrel are encapsulated in various formulations of proniosomal gel composed of various ratios of span surfactant, cholesterol, soya lecithin, and alcohol as aqueous phase prepared by coacervation-phase separation method. The prepared formulations characterized for drug encapsulation efficiency, size distribution, in vitro release studies, and vesicular stability at different storage conditions were carried. Stability studies for proniosomal gel were carried out for a few weeks. Morphological size and shape of the vesicles are characterized using optical microscopy and scanning electron microscopy (SEM). Stability studies for proniosomal gel were carried out for 3 months.

Results: Morphological size and shape of the vesicles are characterized using optical microscopy and SEM, particles are found to be spherical, size of the particles is in the range of 46.4â€“80.6 nm, and permeation studies showed good control release for prolonged period of time. The encapsulation efficiency of proniosomal gel formulations is in the range of 74â€“80% and in vitro permeation studies proved that good amount of drug is permeated and has reasonably good stability characteristics as well.

Conclusions: The results suggest that proniosomal gel formulations of ethinylestradiol and levonorgestrel may be used for transdermal delivery for antifertility treatment. The dried proniosomal formulation could act as a promising alternative to niosomes.

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References

Kakar R, Rao R, Goswami A, Nanda S, Saroha K. Proniosomes: An emerging vesicular system in drug delivery and cosmetics. Der Pharm Lett 2010;2:227-39.

Vyas SP, Khar RK. Novel carrier systems. In: Jain NK, editor. Targeted and Controlled Drug Delivery. New Delhi, India: CBS Publishers and Distributors Pvt Ltd; 2010.

Singh S. Niosomes: A role in targeted drug delivery system. Int J Pharm Sci Res 2013;4:550-7.

Balasubramaniam A, Kumar VA, Pillai KS. Formulation and in vivo evaluation of niosome-encapsulated daunorubicin hydrochloride. Drug Dev Ind Pharm 2002;28:1181-93.

Yoshioka T, Stermberg B, Florence AT. Preparation and properties of vesicles (niosomes) of sobitan monoesters (Span 20, 40, 60, and 80) and a sorbitantristearate (Span 85). Int J Pharm 1994;105:1-6.

Karki R, Mamatha GC, Subramanya G, Udupa N. Preparation, characterization and tissue disposition of niosomes containing isoniazid. Rasayan J Chem 2008;1:224-7.

Tavano L, Infante MR, Riya AM, et al. Role of aggregate size in the hemolytic and antimicrobial activity of colloidal solutions based on single and gemini surfactants from arginine. Soft Matter 2013;9:306-19.

Walker RB, Smith EW. The role of percutaneous penetration enhancers. Adv Drug Deliv Rev 1996;18:295-301.

Paolino D, Muzzalupo R, Ricciardi A, Celia C, Picci N, Fresta M, et al. In vitro and in vivo evaluation of bola-surfactant containing niosomes for transdermal delivery. Biomed Microdevices 2007;9:421-33.

Barry BW. Lipid protein partitioning theory of skin penetration enhancement. J Control Release 1991;15:237-48.

Schreier H, Bouwstra J. Liposomes and niosomes as topical drug carriers: Dermal and transdermal drug delivery. J Control Release 1994;30:1-15.

Touitou E, Dayan N, Bergelson L, Godin B, Eliaz M. Ethosomes-novel vesicular carriers for enhanced delivery: Characterization and skin penetration properties. J Control Release 2000;65:403-18.

Patel KK, Kumar P, Thakkar HP. Formulation of niosomal gel for enhanced transdermal lopinavir delivery and its comparative evaluation with ethosomal gel. AAPS Pharm Sci Tech 2012;13:1502-10.

Ammar HO, Ghorab M, El-Nahhas SA, Higazy IM. Proniosomes as a carrier system for transdermal delivery of tenoxicam. Int J Pharm 2011;405:142-52.

Gupta A, Prajapati SK, Balamurugan M, Singh M, Bhatia D. Design and development of a proniosomal transdermal drug delivery system for captopril. Trop J Pharm Res 2007;6:687-93.

Mishra A, Kapoor AN, Bhargava SH. Proniosomal gel as a carrier for transdermal drug delivery of clotrimazole. Int J Pharm Pharm Sci 2012;4:610-14.

Patil HN, Hardikar SR, Bhosale AV. Formulation development and evaluation of proniosomal gel of carvedilol. Int J Pharm Pharm Sci 2012;4:191-7.

Chauhan BS, Naved T. Herbal contraceptives: Evaluation of antifertility potential of Hibiscus rosa-sinensis (Linn). Asian J Pharm Clin Res 2018;11:36-41.