title: Improving Efficacy, Oral Bioavailability, and Delivery of Paclitaxel Using Protein-Grafted Solid Lipid Nanoparticles.
abstract: Oral delivery of anticancer drugs remains challenging despite the most convenient route of drug administration. Hydrophobicity and nonspecific toxicities of anticancer agents are major impediments in the development of oral formulation. In this study, we developed wheat germ agglutinin (WGA)-conjugated, solid lipid nanoparticles to improve the oral delivery of the hydrophobic anticancer drug, paclitaxel (PTX). This study was focused to improve the PTX loading in biocompatible lipid matrix with high bioconjugation efficiency. WGA-conjugated, PTX-loaded solid lipid nanoparticles (LPSN) exhibited enhanced anticancer activity against A549 lung cancer cells after internalization through lectin receptors than free PTX. Biodistribution studies in rats revealed that LPSN significantly improved the oral bioavailability and lung targetability of PTX, which could be due to cumulative bioadhesive property of the nanocarrier system and the targeting ligand WGA.
authors.affiliation: Medicinal Chemistry & Pharmacology Division, CSIR-Indian Institute of Chemical Technology , Hyderabad, Telangana 500007, India.|Ian Potter NanoBioSensing Facility, NanoBiotechnology Research Laboratory, School of Science, RMIT University , Melbourne, VIC 3001, Australia.|Faculty of Pharmacy, College of Technology, Osmania University , Hyderabad, Telangana 500007, India.
authors.forename: Deep
authors.initials: D
authors.lastname: Pooja
authors.affiliation: Medicinal Chemistry & Pharmacology Division, CSIR-Indian Institute of Chemical Technology , Hyderabad, Telangana 500007, India.|Health Innovations Research Institute, RMIT University , Melbourne, VIC 3083, Australia.|Ian Potter NanoBioSensing Facility, NanoBiotechnology Research Laboratory, School of Science, RMIT University , Melbourne, VIC 3001, Australia.
authors.forename: Hitesh
authors.initials: H
authors.lastname: Kulhari
authors.affiliation: Medicinal Chemistry & Pharmacology Division, CSIR-Indian Institute of Chemical Technology , Hyderabad, Telangana 500007, India.
authors.forename: Madhusudana
authors.initials: M
authors.lastname: Kuncha
authors.affiliation: Faculty of Pharmacy, College of Technology, Osmania University , Hyderabad, Telangana 500007, India.
authors.forename: Shyam S
authors.initials: SS
authors.lastname: Rachamalla
authors.affiliation: Health Innovations Research Institute, RMIT University , Melbourne, VIC 3083, Australia.|Illawarra Health and Medical Research Institute (IHMRI), University of Wollongong , Wollongong, NSW 2522, Australia.
authors.forename: David J
authors.initials: DJ
authors.lastname: Adams
authors.affiliation: Health Innovations Research Institute, RMIT University , Melbourne, VIC 3083, Australia.|Ian Potter NanoBioSensing Facility, NanoBiotechnology Research Laboratory, School of Science, RMIT University , Melbourne, VIC 3001, Australia.
authors.forename: Vipul
authors.initials: V
authors.lastname: Bansal
authors.affiliation: Medicinal Chemistry & Pharmacology Division, CSIR-Indian Institute of Chemical Technology , Hyderabad, Telangana 500007, India.
authors.forename: Ramakrishna
authors.initials: R
authors.lastname: Sistla
mesh_terms: D000072283:A549 Cells; D000818:Animals; D017209:Apoptosis / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D006801:Humans; D008175:Lung Neoplasms / Q000378:metabolism; D053758:Nanoparticles / Q000737:chemistry*; D049329:Nanostructures / Q000737:chemistry; D017239:Paclitaxel / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats
chemical_list: D017239:Paclitaxel
keywords: bioavailability; lung cancer; paclitaxel; solid lipid nanoparticles; wheat germ agglutinin