Investigation of pluronic and PEG-PE micelles as carriers of meso-tetraphenyl porphine for oral administration.
Meso-tetraphenyl porphine (mTPP) is a highly lipophilic, fluorescent porphyrin derivate and it is used as photosensitizer on the treatment of malign neoplasms. The aim of this study was to prepare mTPP loaded pluronic F127 and polyethylene glycol-distearoyl phosphatidylethanolamine (PEG(2000)-DSPE) micelles to evaluate polymeric micelles potential for the transport of drugs through intestinal mucosa. Transport and bioadhesion behaviors of polymeric micelles was investigated using Caco-2 cell monolayer and everted rat intestine models. In order to show that Caco-2 cells can be used as a transport model cytotoxicity of formulations was tested. Cell viability was more than 80%, showing that Caco-2 cells will keep their viability during the transport studies demonstrating that prepared formulations can be securely used as oral drug carrier systems. Plain micelles were labeled with a fluorescent agent rhodamine-phosphatidylethanolamine (Rh-PE) and their transport through Caco-2 cells was investigated beside mTPP loaded micelles. At the end of 4h transport study through Caco-2 cells, cumulative transport (%) of fluorescent agents were around 14% and 1% in Rh-PE labeled and mTPP loaded micelles This difference was attributed to the different placement of mTPP and Rh-PE in the micellar core. Drug transport was not estimated in everted rat intestine model but the bioadhesion was 79% and 70% for mTPP loaded pluronic F127 and PEG(2000)-DSPE micelles. These good bioadhesion rates are promising for oral drug delivery.
Sezgin
Zerrin
Z
Ankara University, School of Pharmacy, Department of Pharmaceutical Technology, 06100 Tandogan, Ankara, Turkey.
Yuksel
Nilufer
N
Baykara
Tamer
T
D000284:Administration, Oral; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism* / Q000633:toxicity; D018938:Caco-2 Cells; D002470:Cell Survival / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers; D004339:Drug Compounding; D017097:Electric Impedance; D006801:Humans; D066298:In Vitro Techniques; D007408:Intestinal Absorption; D007413:Intestinal Mucosa / Q000378:metabolism*; D008297:Male; D008823:Micelles; D010714:Phosphatidylethanolamines / Q000737:chemistry* / Q000633:toxicity; D017319:Photosensitizing Agents / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism* / Q000633:toxicity; D020442:Poloxamer / Q000737:chemistry* / Q000633:toxicity; D011092:Polyethylene Glycols / Q000737:chemistry* / Q000633:toxicity; D011166:Porphyrins / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism* / Q000633:toxicity; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D013997:Time Factors; D000267:Tissue Adhesions
D000970:Antineoplastic Agents; D004337:Drug Carriers; D008823:Micelles; D010714:Phosphatidylethanolamines; D017319:Photosensitizing Agents; D011166:Porphyrins; D020442:Poloxamer; C067972:dioleoyl-N-(monomethoxypolyethylene glycol succinyl)phosphatidylethanolamine; D011092:Polyethylene Glycols; C049692:tetraphenylporphine