title: The utility of self-emulsifying oil formulation to improve the poor solubility of the anti HIV drug CSIC.
abstract: BACKGROUND
  CSIC (5-chloro-3-phenylsulfonylindole-2-carboxamide), a non-nucleoside reverse transcriptase inhibitor (NNRTI) has not been advanced as a therapeutic anti-HIV candidate drug due to its low aqueous solubility and poor bioavailability.
  
  
  OBJECTIVE
  The objective of this work was to formulate CSIC into self-emulsifying oil formulations for the purpose of improving its aqueous solubility and evaluating in vitro antiretroviral activity.
  
  
  METHODS
  CSIC self-emulsifying oil formulations (SEFs) were formulated and evaluated for droplet size, zeta potential, polydispersity index (PDI), viscosity, emulsification time, stability and bioactivity.
  
  
  RESULTS
  Results showed significantly improved solubility of CSIC in the SEFs.The concentration of co-surfactant affected the droplet size, zeta potential and polydispersity index. In vitro bioactivity studies showed that the CSIC SEFs retained full anti-HIV activity.
  
  
  CONCLUSIONS
  The in vitro data from this first attempt to formulate CSIC SEFs suggest that improvement on the aqueous solubility of CSIC through this delivery system may accentuate its antiretroviral effectiveness in vivo via bioavailability enhancement. The formulation is therefore intended as an oral anti-HIV agent for prophylactic and therapeutic uses.
authors.affiliation: Department of Pharmaceutical Technology and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Nigeria. obittenick@yahoo.com.
authors.forename: Nicholas C
authors.initials: NC
authors.lastname: Obitte
authors.forename: Lisa C
authors.initials: LC
authors.lastname: Rohan
authors.forename: Christianah M
authors.initials: CM
authors.lastname: Adeyeye
authors.forename: Michael A
authors.initials: MA
authors.lastname: Parniak
authors.forename: Charles O
authors.initials: CO
authors.lastname: Esimone