Lipid-based dispersions of exemestane for improved dissolution rate and intestinal permeability: in vitro and ex vivo characterization.
Current study aimed to develop lipid dispersions of poorly water soluble exemestane by employing lipid carriers such as Gelucire 44/14 and TPGS with porous calcium silicate (PCS) as an adsorbent carrier and formulate into a solid dosage form. The lipid dispersions at 1:5 ratio showed the highest solubility and dissolution compared to pure exemestane. Further, the ex vivo intestinal permeation studies showed improved apparent permeability (Papp, cm/s) of exemestane from the lipid dispersions (GLD1:51.3 × 10-2cm/s; TLD1:51.8 × 10-2cm/s) compared to pure exemestane (0.7 × 10-2cm/s). The optimized lipid dispersions (GLD1:5and TLD1:5) were evaluated for scalability to develop into capsules.
a Department of Pharmaceutics , St. Peter's Institute of Pharmaceutical Sciences , Vidyanagar, Warangal , Telangana , India.
Basanth Babu
BB
Eedara
a Department of Pharmaceutics , St. Peter's Institute of Pharmaceutical Sciences , Vidyanagar, Warangal , Telangana , India.
Suresh
S
Bandari
D000730:Androstadienes / Q000737:chemistry* / Q000378:metabolism*; D017610:Calcium Compounds / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry*; D007413:Intestinal Mucosa / Q000378:metabolism*; D008055:Lipids / Q000737:chemistry*; D010539:Permeability; D011092:Polyethylene Glycols / Q000737:chemistry; D017640:Silicates / Q000737:chemistry; D012995:Solubility; D014810:Vitamin E / Q000737:chemistry
D000730:Androstadienes; D017610:Calcium Compounds; D004337:Drug Carriers; D008055:Lipids; D017640:Silicates; C104509:gelucire 44-14; D014810:Vitamin E; D011092:Polyethylene Glycols; C056516:exemestane; C014225:tocophersolan; C031293:calcium silicate
Dissolution; Gelucire 44/14; exemestane; lipid dispersions; permeability; vitamin E TPGS