title: Proliposome powders for enhanced intestinal absorption and bioavailability of raloxifene hydrochloride: effect of surface charge.
abstract: The primary goal of the present study was to investigate the combined prospective of proliposomes and surface charge for the improved oral delivery of raloxifene hydrochloride (RXH). Keeping this objective, the present systematic study was focused to formulate proliposomes by varying the ratio of hydrogenated soyphosphatidylcholine and cholesterol. Furthermore, to assess the role of surface charge on improved absorption of RXH, anionic and cationic vesicles were prepared using dicetyl phosphate and stearylamine, respectively. The formulations were characterized for size, zeta potential and entrapment efficiency. The improved dissolution characteristics assessed from dissolution efficiency, mean dissolution rate were higher for proliposome formulations. The solid state characterization studies indicate the transformation of native crystalline form of the drug to amorphous and/or molecular state. The higher effective permeability coefficient and fraction absorbed in humans extrapolated from in situ single-pass intestinal absorption study data in rats provide an insight on the potential of proliposomes and cationic surface charge for augment in absorption across gastro intestinal barrier. To draw the conclusions, in vivo pharmacokinetic study carried out in rats indicate a threefold enhancement in the rate and extent of absorption of RXH from cationic proliposome formulation which unfurl the potential of proliposomes and role of cationic charge for improved oral delivery of RXH.
authors.affiliation: Department of Pharmaceutics, St. Peter's Institute of Pharmaceutical Sciences , Warangal , India.
authors.forename: Ashok
authors.initials: A
authors.lastname: Velpula
authors.forename: Raju
authors.initials: R
authors.lastname: Jukanti
authors.forename: Karthik Yadav
authors.initials: KY
authors.lastname: Janga
authors.forename: Sharath
authors.initials: S
authors.lastname: Sunkavalli
authors.forename: Suresh
authors.initials: S
authors.lastname: Bandari
authors.forename: Prabhakar
authors.initials: P
authors.lastname: Kandadi
authors.forename: Prabhakar Reddy
authors.initials: PR
authors.lastname: Veerareddy
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000838:Anions; D001682:Biological Availability; D002412:Cations; D002784:Cholesterol / Q000737:chemistry; D003460:Crystallization; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D006801:Humans; D007408:Intestinal Absorption; D008081:Liposomes; D008297:Male; D010316:Particle Size; D010713:Phosphatidylcholines / Q000737:chemistry; D011208:Powders; D020849:Raloxifene Hydrochloride / Q000008:administration & dosage / Q000493:pharmacokinetics*; D051381:Rats; D017208:Rats, Wistar; D020845:Selective Estrogen Receptor Modulators / Q000008:administration & dosage / Q000493:pharmacokinetics*; D012995:Solubility; D013025:Glycine max / Q000737:chemistry
chemical_list: D000838:Anions; D002412:Cations; D004337:Drug Carriers; D008081:Liposomes; D010713:Phosphatidylcholines; D011208:Powders; D020845:Selective Estrogen Receptor Modulators; D020849:Raloxifene Hydrochloride; D002784:Cholesterol