Formulation development for solubility and dissolution enhancement of an Anti-Retroviral Drug as nanocrystal suspension using high pressure homogenization

Rajveer Bhaskar, Prakash H Patil


Efavirenz is a non-nucleoside reverse transcriptase inhibitor and categorized in to BCS class II drug. Efavirenz exhibit low and variable bioavailability due to its poor aqueous solubility. So, it needs enhancement in the solubility, dissolution rate and bioavailability to derive its maximum therapeutic efficacy. The aim of the present investigation was to enhance the solubility, dissolution and stability of nanocrystal suspension of efavirenz using a non-ionic stabilizer. Nanocrystal suspensions were prepared by high pressure homogenization technique and evaluated for particle size, poly dispersity index, zeta potential, and drug release. Particles with average size of 251.3 nm, having PDI of 0.214 were produced. Zeta potential was found to be −31.2 mV and the formulation was found stable on the basis of results obtained from differential scanning calorimetry and powder X-ray diffraction studies. The drug release revealed enhanced permeation of drug, as desired, indicating its potential for an attempt towards successful nanocrystal formulation.

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