SOLUBILITY ENHANCEMENT OF SELEXIPAG BY β-CYCLODEXTRIN INCLUSION COMPLEXES

Celse Kwitonda; Sonam Choki; Kule Gift Diadone

doi:10.22270/ujpr.v11i2.1529

Celse Kwitonda Department of Pharmaceutical Science, Marwadi University, Rajkot, Gujarat, India.
Sonam Choki Department of Pharmaceutical Science, Marwadi University, Rajkot, Gujarat, India.
Kule Gift Diadone Department of Pharmaceutical Science, Marwadi University, Rajkot, Gujarat, India.

10.22270/ujpr.v11i2.1529

Keywords:

Cyclodextrins, inclusion complexes, kneading, pulmonary arterial hypertension, solubility enhancement

Abstract

Background: Selexipag is an oral, non-prostanoid IP receptor agonist used in treating pulmonary arterial hypertension (PAH). Selexipag has poor aqueous solubility, especially in acidic solution medium. Hence, for the purposes of overcoming solubility limitations associated with selexipag, various techniques such as complexation with appropriate complexing agents have been considered. Cyclodextrins are unique molecules that are cyclic carbohydrates that have been shown to be suitable for the purpose of inclusion complex formation. This is because they form inclusion complexes when combined with insoluble drugs.

Method: The inclusion complex between Selexipag and β-cyclodextrin was prepared using kneading method.

Result: The ability of β-cyclodextrin to increase the solubility of Selexipag has been shown from the results indicating that β-cyclodextrin improves significantly both the solubility and dissolution of selexipag which is a poorly soluble drug. The formation of the inclusion complex was further confirmed using UV-visible spectrophotometry and Fourier transform infrared spectroscopy. In addition, dissolution studies indicated improved dissolution behavior of the complexed drug.

Conclusion: From the results obtained above, β-cyclodextrin appears to be very efficient carrier agent for poorly soluble drugs such as Selexipag which belong to BCS class II.