title: Lipopolysaccharide based oral nanocarriers for the improvement of bioavailability and anticancer efficacy of curcumin.
abstract: Soluthin MD(®), a unique phosphatidylcholine-maltodextrin based hydrophilic lipopolysaccharide, which exhibits superior biocompatibility and bioavailability enhancer properties for poorly water soluble drug(s). Curcumin (CUR) is a potential natural anticancer drug with low bioavailability due to poor aqueous solubility. The study aims at formulation and optimization of CUR loaded lipopolysaccharide nanocarriers (C-LPNCs) to enhance oral bioavailability and anticancer efficacy in colon-26 tumor-bearing mice in vitro and in vivo. The Optimized C-LPNCs demonstrated favorable mean particle size (108 ± 3.4 nm) and percent entrapment efficiency (65.29 ± 1.0%). Pharmacokinetic parameters revealed ∼130-fold increase in oral bioavailability and cytotoxicity studies demonstrated ∼23-fold reduction in 50% cell growth inhibition when treated with optimized C-LPNCs as compared to pure CUR. In vivo anticancer study performed with optimized C-LPNCs showed significant increase in efficacy compared with pure CUR. Thus, lipopolysaccharide nanocarriers show potential delivery strategy to improve oral bioavailability and anticancer efficacy of CUR in the treatment of colorectal cancer.
authors.affiliation: Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi 221 005, UP, India.
authors.forename: Sundeep
authors.initials: S
authors.lastname: Chaurasia
authors.affiliation: Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi 221 005, UP, India.
authors.forename: Ravi R
authors.initials: RR
authors.lastname: Patel
authors.affiliation: Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi 221 005, UP, India.
authors.forename: Pramila
authors.initials: P
authors.lastname: Chaubey
authors.affiliation: Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi 221 005, UP, India.
authors.forename: Nagendra
authors.initials: N
authors.lastname: Kumar
authors.affiliation: Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi 221 005, UP, India.
authors.forename: Gayasuddin
authors.initials: G
authors.lastname: Khan
authors.affiliation: Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi 221 005, UP, India. Electronic address: bmishrabhu@rediffmail.com.
authors.forename: Brahmeshwar
authors.initials: B
authors.lastname: Mishra
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D001682:Biological Availability; D003474:Curcumin / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry*; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D005260:Female; D006801:Humans; D008070:Lipopolysaccharides / Q000737:chemistry*; D008297:Male; D008807:Mice, Inbred BALB C; D049329:Nanostructures / Q000737:chemistry; D010316:Particle Size; D017208:Rats, Wistar
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D004337:Drug Carriers; D008070:Lipopolysaccharides; D003474:Curcumin
keywords: Bioavailability; Colorectal cancer; Curcumin (PubChem CID: 969516); Cytotoxicity; Lipopolysaccharide; Nanocarriers