Bioavailability enhancement, Caco-2 cells uptake and intestinal transport of orally administered lopinavir-loaded PLGA nanoparticles.
Nanoparticles (NPs) can be absorbed via M cells of Peyer's patches after oral delivery leading to passive lymphatic targeting followed by systemic drug delivery. Hence, the study was aimed to formulate PLGA NPs of lopinavir. The NPs were prepared by nanoprecipitation, optimized by 33factorial design and characterized by TEM, DSC, FTIR studies and safety was assessed by MTT assay. In vivo pharmacokinetic studies were performed in rats. The NPs were discrete spherical structures having particle size of 142.1 ± 2.13 nm and entrapment of 93.03 ± 1.27%. There was absence of drug-polymer interaction. Confocal images revealed the penetration and absorption of coumarin-loaded NPs in Caco-2 cells and intestine after oral delivery. There was 3.04 folds permeability and 13.9 folds bioavailability enhancement from NPs. The NPs can be promising delivery system for antiretroviral drug by delivering the drug to lymph (major HIV reservoir site) via direct absorption through intestine before reaching systemic circulation.
a Pharmacy Department, TIFAC Centre of Relevance and Excellence in NDDS, Centre for PG Studies and Research, M S University of Baroda , Vadodara , Gujarat , India.
Garima
G
Joshi
a Pharmacy Department, TIFAC Centre of Relevance and Excellence in NDDS, Centre for PG Studies and Research, M S University of Baroda , Vadodara , Gujarat , India.
Abhinesh
A
Kumar
a Pharmacy Department, TIFAC Centre of Relevance and Excellence in NDDS, Centre for PG Studies and Research, M S University of Baroda , Vadodara , Gujarat , India.
Krutika
K
Sawant
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D018938:Caco-2 Cells; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods; D006801:Humans; D007408:Intestinal Absorption / Q000502:physiology; D007413:Intestinal Mucosa / Q000378:metabolism*; D019344:Lactic Acid / Q000737:chemistry*; D061466:Lopinavir / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism*; D008297:Male; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism*; D010316:Particle Size; D010539:Permeability; D010581:Peyer's Patches / Q000737:chemistry / Q000378:metabolism; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D051381:Rats; D017208:Rats, Wistar
D004337:Drug Carriers; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D061466:Lopinavir; D011100:Polyglycolic Acid; D019344:Lactic Acid
Intestinal uptake; lopinavir; lymphatic delivery; nanoparticles; oral administration; pharmacokinetics