Formulation development and in vitro evaluation of didanosine-loaded nanostructured lipid carriers for the potential treatment of AIDS dementia complex.

Abstract

The purpose of this article was to investigate the feasibility of incorporating didanosine (DDI) into nanostructured lipid carriers (NLC) for potential treatment of AIDS dementia complex. Aqueous DDI-free and DDI-loaded NLC were manufactured using hot high-pressure homogenization. The lipid matrix contained a mixture of Precirol® ATO 5 and Transcutol® HP. Photon correlation spectroscopy revealed that the mean particle size for all formulations was below 250 nm with narrow polydispersity indices. In addition, the d99% values for all formulations determined using laser diffractometry were below 400 nm with the span values ranging from 0.84 to 1.0. The zeta potential values ranged from -18.4 to -11.4 mV and the encapsulation efficiency of NLC for DDI ranged from 33.02% to 78.34%. These parameters remained relatively constant for all formulations tested following storage for 2 months at 25°C indicating that all the formulations were relatively stable. Differential scanning calorimetry revealed a decrease in the degree of crystallinity of NLC in all formulations developed relative to the bulk lipid material. In addition, wide-angle X-ray scattering showed that NLC in all formulations tested existed in a single β-modification form and that DDI that had been incorporated into the NLC appeared to be molecularly dispersed in the lipid matrices. Images of the NLC formulations obtained using transmission electron microscopy revealed that all formulations contained a mixture of spherical and nonspherical particles irrespective of the amount of DDI that was added during the manufacture of the formulations.

• Authors: Kasongo Wa Kasongo, Ranjita Shegokar, Rainer H Müller, Roderick B Walker
• Journal: Drug development and industrial pharmacy (Drug Dev Ind Pharm) Vol. 37 Issue 4 Pg. 396-407 (Apr 2011) ISSN: 1520-5762 [Electronic] England
• PMID: 20923388 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Drug Carriers
• Lipids
• Didanosine

Topics

• AIDS Dementia Complex (drug therapy)
• Chemistry, Pharmaceutical
• Crystallization
• Didanosine (administration & dosage, chemistry)
• Drug Carriers
• Humans
• Lipids (administration & dosage)
• Microscopy, Electron, Transmission
• Nanostructures
• Pressure