Dissolution enhancement of efavirenz by solid dispersion and PEGylation techniques.
BACKGROUND
Efavirenz is the preferred nonnucleotide reverse transcriptase inhibitor for first-line antiretroviral treatment in many countries. It is orally active and is specific for human immunodeficiency virus type 1. Its effectiveness can be attributed to its long half-life, which is 52-76 h after multiple doses. The drug is having poor water solubility. The formulation of poorly soluble drug for oral delivery will be one of the biggest challenges for formulation scientists in the research field. Among the available approaches, the solid dispersion technique has often proved to be the most commonly used method in improving dissolution and bioavailability of the drugs because of its simplicity and economy in preparation and evaluation.


METHODS
Solid dispersions were prepared by solvent evaporation and physical mixture methods by using polyethylene glycol as the hydrophilic carrier and PEGylated product was also prepared. The prepared products were evaluated for various parameters, such as polymer interaction, saturation solubility study, and drug release studies. The drug release data were analyzed by fitting it into various kinetic models.


RESULTS
There is an improvement in the dissolution from 16% to 70% with solid dispersion technology. Higuchi model was found to be the best fit model.


CONCLUSIONS
Solid dispersion is the simple, efficient, and economic method to improve the dissolution of the poorly water-soluble drugs.
Department of Pharmacy, Faculty of Technology, Osmania University, Hyderabad, India.
B Bindu
BB
Madhavi
B
B
Kusum
Ch Krishna
ChK
Chatanya
M Naga
MN
Madhu
V Sri
VS
Harsha
David
D
Banji