NDLI: Enhanced Corneal Absorption of Erythromycin by Modulating P-Glycoprotein and MRP Mediated Efflux with Corticosteroids

Content Provider	Springer Nature Link
Author	Hariharan, Sudharshan Gunda, Sriram Mishra, Gyan P. Pal, Dhananjay Mitra, Ashim K.
Copyright Year	2008
Abstract	The objectives were (i) to test in vivo functional activity of MRP2 on rabbit corneal epithelium and (ii) to evaluate modulation of P-gp and MRP2 mediated efflux of erythromycin when co-administered with corticosteroids.Cultured rabbit primary corneal epithelial cells (rPCECs) was employed as an in vitro model for rabbit cornea. Cellular accumulation and bi-directional transport studies were conducted across Madin-Darby Canine Kidney (MDCK) cells overexpressing MDR1 and MRP2 proteins to delineate transporter specific interaction of steroids. Ocular pharmacokinetic studies were conducted in rabbits following a single-dose infusion of erythromycin in the presence of specific inhibitors and steroids.Bi-directional transport of erythromycin across MDCK-MDR1 and MDCK-MRP2 cells showed significant difference between BL-AP and AP-BL permeability, suggesting that erythromycin is a substrate for P-gp and MRP2. Cellular accumulation of erythromycin in rPCEC was inhibited by steroids in a dose dependent manner. MK571, a specific MRP inhibitor, modulated the aqueous humor concentration of erythromycin in vivo. Even, steroids inhibited P-gp and MRP2 mediated efflux with maximum increase in k $_{a}$, AUC$_{0 − ∞}$, C $_{max}$ and C $_{last}$ values of erythromycin, observed with 6α-methyl prednisolone.MRP2 is functionally active along with P-gp in effluxing drug molecules out of corneal epithelium. Steroids were able to significantly inhibit both P-gp and MRP2 mediated efflux of erythromycin.
Starting Page	1270
Ending Page	1282
Page Count	13
File Format	PDF
ISSN	07248741
Journal	Pharmaceutical Research
Volume Number	26
Issue Number	5
e-ISSN	1573904X
Language	English
Publisher	Springer US
Publisher Date	2008-10-29
Publisher Place	Boston
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Biomedical Engineering Medical Law Biochemistry Pharmacy Pharmacology/Toxicology
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Pharmacology Molecular Medicine Pharmacology (medical) Biotechnology Pharmaceutical Science

Sl.	Authority	Responsibilities	Communication Details
1	Ministry of Education (GoI), Department of Higher Education	Sanctioning Authority	https://www.education.gov.in/ict-initiatives
2	Indian Institute of Technology Kharagpur	Host Institute of the Project: The host institute of the project is responsible for providing infrastructure support and hosting the project	https://www.iitkgp.ac.in
3	National Digital Library of India Office, Indian Institute of Technology Kharagpur	The administrative and infrastructural headquarters of the project	Dr. B. Sutradhar bsutra@ndl.gov.in
4	Project PI / Joint PI	Principal Investigator and Joint Principal Investigators of the project	Dr. B. Sutradhar bsutra@ndl.gov.in Prof. Saswat Chakrabarti will be added soon
5	Website/Portal (Helpdesk)	Queries regarding NDLI and its services	support@ndl.gov.in
6	Contents and Copyright Issues	Queries related to content curation and copyright issues	content@ndl.gov.in
7	National Digital Library of India Club (NDLI Club)	Queries related to NDLI Club formation, support, user awareness program, seminar/symposium, collaboration, social media, promotion, and outreach	clubsupport@ndl.gov.in
8	Digital Preservation Centre (DPC)	Assistance with digitizing and archiving copyright-free printed books	dpc@ndl.gov.in
9	IDR Setup or Support	Queries related to establishment and support of Institutional Digital Repository (IDR) and IDR workshops	idr@ndl.gov.in

Enhanced Corneal Absorption of Erythromycin by Modulating P-Glycoprotein and MRP Mediated Efflux with Corticosteroids

Mdr1 Transfection Causes Enhanced Apoptosis by Paclitaxel: An Effect Independent of Drug Efflux Function of P-Glycoprotein

Evidence for Modulation of P-glycoprotein-Mediated Efflux by Methoxypolyethylene Glycol-block-Polycaprolactone Amphiphilic Diblock Copolymers

P-glycoprotein (P-gp/MDR1)-Mediated Efflux of Sex-Steroid Hormones and Modulation of P-gp Expression In Vitro

Compartmental Models for Apical Efflux by P-glycoprotein—Part 1: Evaluation of Model Complexity

Grapefruit Juice Activates P-Glycoprotein-Mediated Drug Transport

Structural Determinants of P-Glycoprotein-Mediated Transport of Glucocorticoids

Enhanced Oral Bioavailability of Paclitaxel by Coadministration of the P-Glycoprotein Inhibitor KR30031

Compartmental Models for Apical Efflux by P-glycoprotein: Part 2—A Theoretical Study on Transporter Kinetic Parameters

Enhanced Corneal Absorption of Erythromycin by Modulating P-Glycoprotein and MRP Mediated Efflux with Corticosteroids

Similar Documents

Enhanced Corneal Absorption of Erythromycin by Modulating P-Glycoprotein and MRP Mediated Efflux with Corticosteroids

Mdr1 Transfection Causes Enhanced Apoptosis by Paclitaxel: An Effect Independent of Drug Efflux Function of P-Glycoprotein

Evidence for Modulation of P-glycoprotein-Mediated Efflux by Methoxypolyethylene Glycol-block-Polycaprolactone Amphiphilic Diblock Copolymers

P-glycoprotein (P-gp/MDR1)-Mediated Efflux of Sex-Steroid Hormones and Modulation of P-gp Expression In Vitro

Compartmental Models for Apical Efflux by P-glycoprotein—Part 1: Evaluation of Model Complexity

Grapefruit Juice Activates P-Glycoprotein-Mediated Drug Transport

Structural Determinants of P-Glycoprotein-Mediated Transport of Glucocorticoids

Enhanced Oral Bioavailability of Paclitaxel by Coadministration of the P-Glycoprotein Inhibitor KR30031

Compartmental Models for Apical Efflux by P-glycoprotein: Part 2—A Theoretical Study on Transporter Kinetic Parameters

Enhanced Corneal Absorption of Erythromycin by Modulating P-Glycoprotein and MRP Mediated Efflux with Corticosteroids