Abstract

FORMULATION AND EVALUATION OF NANOEMULSION VAGINAL SUPPOSITORIES OF PROGESTERONE FOR PCOS

Rahul Kumar*, Raj Kumar Mishra and Dr. Pushpendra Jain

ABSTRACT

In present research work, nanoemulsions with different ratio of oil, surfactant and water containing co-surfactant were prepared as a carrier loaded with progesterone and incorporated in gelatin based suppositories. It is stated that Progesterone is a natural steroid hormone. Currently, it is used to promote fertility and also has been prescribed for induction amenorrhoea, regular bleeding, and subatrophy or full secretory changes of the endometrium, by modifying the dose, duration of treatment and the route of administration. Progesterone can be administered by different routes: oral, vaginal and intramuscular and, recently, subcutaneous. Each of these routes has different effects in supporting the luteal phase. However, orally delivered progesterone is rapidly cleared by first-pass hepatic metabolism and this result in poor bioavailability. The developed nanoemulsion formed from Capmul MCM, Kolliphor EL and Transcutol HP is a promising approach to improve the solubility of Progesterone because of the simple manufacturing process, low production costs and the possibility of manufacturing at industrial scale. The resulted formulation has shown particles size of 82.85 nm and polydispersity index of 0.262. The zeta potential of nanoemulsion was -28.8 mV, indicated good stability of the formulation. Nanoemulsion developed was clear and transparent, with pH 5.8 and drug content was found to be 99.98±0.232%. The novel nanoemulsion loaded gelatin based suppositories of progesterone with uniform weight (0.320±1.377 gm to 0.928±0.882 gm) and content (48.575±0.123% to 54.569±0.246%) was successfully formulated for vaginal route. The prepared suppository formulations exhibited hardness ranging from 4.6 to 7.3 kg which ensures the ability to withstand pressure during handling, shipping and insertion. The suppository formulations A1-A3 has 8- 9 min of disintegration time which complies with acceptance limit for water soluble suppositories i.e within 60 minutes. The in-vitro release study of formulation code A2 containing progesterone loaded nanoemulsion has shown maximum drug release as compare to market formulation up to 51.723±0.085% within 2 hr. It was found that in vitro drug release of A2 Formulation was best explained by higuchi model as the plot showed the highest R2 value which indicates the sustain release of the progesterone through the suppository.

Keywords: Nanoemulsion, progesterone, gelatine suppository, disintegration time.