The utility of self-emulsifying oil formulation to improve the poor solubility of the anti HIV drug CSIC

نویسندگان

  • Nicholas C Obitte
  • Lisa C Rohan
  • Christianah M Adeyeye
  • Michael A Parniak
  • Charles O Esimone
چکیده

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. CONCLUSION 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.

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Design, Development and In Vitro Characterization of Self Emulsifying Drug Delivery System for Irbesartan

The objectives of present investigations were to optimize concentration of oil, surfactant and cosurfactant by pseudoternary phase diagrams and to develop a stable formulation of self emulsifying drug delivery system (SEDDS) in order to enhance the dissolution rate of poorly soluble Irbesartan (IBS) by SEDDS. Pseudoternary phase diagrams were constructed to identify the self emulsifying region....

متن کامل

Development, Characterization and Optimization of Ibuprofen Self-emulsifying Drug Delivery System Applying Face Centered Experimental Design

Ibuprofen (IB) a NSAID, has poor dissolution and many gastrointestinal side effects. Self-Emulsifying drug delivery system (SEDDS) has proved its efficacy to improve the solubility and dissolution of many lipophilic drugs and improve their characteristics. The objectives of this study were to develop, optimize and characterize a IBSEDDS applying Face Centered Experimental Design (FCED). The met...

متن کامل

Development of Solid Self Emulsifying Drug Delivery Systems Containing Efavirenz: in Vitro and in Vivo Evaluation

Efavirenz is a drug with an absorption window. Its oral bioavailability is 40-50%. The aim of this work was to formulate solid self-emulsifying drug delivery system to improve the solubility and bioavailability of efavirenz. Solubility of Efavirenz was determined in various vehicles like oils, surfactants and co surfactants. Which, upon dilution with aqueous media, spontaneously form fine oil i...

متن کامل

Self Nano Emulsifying Drug Delivery Systems for Oral Delivery of Hydrophobic Drugs

Self-emulsifying drug delivery systems (SNEDDS) are highly in quest due to their innumerable benefits like better portability, improved stability and higher drug loading, coupled with ease and economy of their production. SNEDDS are used to improve the solubility of high lipophilic drugs. SNEDDS are improving the oral bioavailability of limited water-soluble drug compounds. These SNEDDS are iso...

متن کامل

Self-emulsifying drug delivery systems as a tool to improve solubility and bioavailability of resveratrol.

Resveratrol is a nonflavonoid polyphenolic compound which has a broad range of desirable biological actions which include antioxidant, anti-inflammatory, antidiabetic, cardioprotective, and antitumor activities. However, there is concern that the bioavailability of resveratrol may limit some of its clinical utility. So, the aim of this study was to enhance the dissolution rate and oral hypoglyc...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

عنوان ژورنال:

دوره 10  شماره 

صفحات  -

تاریخ انتشار 2013