| Autor: |
Madgulkar AR; AISSMS College of Pharmacy, Pune, Maharashtra, 411001, India. armadgulkar@gmail.com., Bhalekar MR; AISSMS College of Pharmacy, Pune, Maharashtra, 411001, India., Kadam AA; AISSMS College of Pharmacy, Pune, Maharashtra, 411001, India. |
| Jazyk: |
angličtina |
| Zdroj: |
AAPS PharmSciTech [AAPS PharmSciTech] 2018 Jan; Vol. 19 (1), pp. 293-302. Date of Electronic Publication: 2017 Jul 17. |
| DOI: |
10.1208/s12249-017-0834-x |
| Abstrakt: |
Lopinavir is a BCS Class IV drug exhibiting poor bioavailability due to P-gp efflux and limited permeation. The aim of this research was to formulate and characterize microspheres of lopinavir using thiolated xyloglucan (TH-MPs) as carrier to improve its oral bioavailability without co-administration of ritonavir. Thiomeric microspheres were prepared by ionotropic gelation between alginic acid and calcium ions. Interaction studies were performed using Fourier transform infrared spectroscopy (FT-IR). The thiomeric microspheres were characterized for its entrapment efficiency, T 80 , surface morphology, and mucoadhesion employing in vitro wash off test. The microspheres were optimized by 3 2 factorial design. The optimized thiomeric microsphere formulation revealed 93.12% entrapment efficiency, time for 80% drug release (T 80 ) of 358.1 min, and 88% mucoadhesion after 1 h. The permeation of lopinavir from microspheres was enhanced 3.15 times as determined by ex vivo study using everted chick intestine and increased relative bioavailability over 3.22-fold over combination of lopinavir and ritonavir as determined by in vivo study in rat model. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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