Mixed-micellar proliposomal systems for enhanced oral delivery of progesterone.
The objective of our study was to develop a mixed-micellar proliposomal formulation of poorly water-soluble drug progesterone and evaluate the dissolution profile and membrane transport. Several formulations of proliposomes were prepared by mixing different concentrations of lipid, progesterone, polysorbate 80, and microcrystalline cellulose. The mixed-micellar formulation of drug:dimyristoyl-phosphatidycholine:polysorbate 80 (1:20:3.3) exhibited the maximum dissolution (75.27%), while pure progesterone resulted in low dissolution. The above formulation showed a 4-fold increase in transport in Caco-2 cells and a 6-fold increase in transport across the everted rat intestinal sac experiments compared with control. Proliposomal formulations enhance the extent of dissolution and membrane transport of progesterone and serve as ideal carriers for oral delivery of drugs with low water solubility.
College of Pharmacy, Western University of Health Sciences, Pomona, California 91766, USA.
Praveen
P
Potluri
Guru V
GV
Betageri
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D001692:Biological Transport; D018938:Caco-2 Cells; D002152:Calorimetry, Differential Scanning; D002482:Cellulose / Q000737:chemistry; D004134:Dimyristoylphosphatidylcholine / Q000737:chemistry; D004337:Drug Carriers / Q000138:chemical synthesis* / Q000737:chemistry; D005079:Excipients / Q000737:chemistry; D006801:Humans; D007413:Intestinal Mucosa / Q000378:metabolism; D008081:Liposomes / Q000138:chemical synthesis / Q000737:chemistry; D008823:Micelles; D010316:Particle Size; D010713:Phosphatidylcholines / Q000737:chemistry; D011136:Polysorbates / Q000737:chemistry; D011374:Progesterone / Q000008:administration & dosage* / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley
D004337:Drug Carriers; D005079:Excipients; D008081:Liposomes; D008823:Micelles; D010713:Phosphatidylcholines; D011136:Polysorbates; D011374:Progesterone; D002482:Cellulose; C109691:microcrystalline cellulose; D004134:Dimyristoylphosphatidylcholine