Entrapment and release of saquinavir using novel cationic solid lipid nanoparticles.
Cationic solid lipid nanoparticles (CSLNs) with entrapped saquinavir (SQV) were fabricated by microemulsion method. Here, CSLNs were stabilized by polysorbate 80, and the lipid phase contained cationic stearylamine (SA) and dioctadecyldimethyl ammonium bromide (DODAB) and nonionic Compritol 888 ATO (CA) and cacao butter (CB). Properties of the present pharmaceutical formulations including the entrapment efficiency, the release kinetics, and the distribution of SQV in CSLNs were analyzed. The results indicated that a mixture of SA and DODAB and a mixture of CA and CB were beneficial to the entrapment efficiency of SQV. However, an increase in the content of cationic lipids insignificantly affected the entrapment efficiency of SQV when the weight percentage of SA and DODAB was greater than 1% during emulsification. Also, the rate of SQV released from CSLNs with lipid cores of a mixture of CA and CB was slower than that of pure CB. The temporal variation in the released SQV suggested that the carriers could be sustained delivery systems with no apparent initial burst. Hence, the current CSLNs could carry SQV for the improved medication of individuals infected by human immunodeficiency viruses.
Kuo
Yung-Chih
YC
Department of Chemical Engineering, National Chung Cheng University, Chia-Yi 62102, Taiwan, ROC. chmyck@ccu.edu.tw
Chen
Hung-Hao
HH
D000588:Amines / Q000737:chemistry; D002099:Cacao / Q000737:chemistry; D002412:Cations / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry*; D004655:Emulsions; D005079:Excipients / Q000737:chemistry*; D005227:Fatty Acids / Q000737:chemistry; D017320:HIV Protease Inhibitors / Q000737:chemistry*; D008055:Lipids / Q000737:chemistry; D053758:Nanoparticles; D011136:Polysorbates / Q000737:chemistry; D000644:Quaternary Ammonium Compounds / Q000737:chemistry; D019258:Saquinavir / Q000737:chemistry*
D000588:Amines; D002412:Cations; D004337:Drug Carriers; D004655:Emulsions; D005079:Excipients; D005227:Fatty Acids; D017320:HIV Protease Inhibitors; D008055:Lipids; D011136:Polysorbates; D000644:Quaternary Ammonium Compounds; C086409:glyceryl behenate; C015831:dimethyldioctadecylammonium; C009317:stearylamine; D019258:Saquinavir