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The emerging role of P-glycoprotein inhibitors in drug delivery: a patent review

  作者 Akhtar, N; Ahad, A; Khar, RK; Jaggi, M; Aqil, M; Iqbal, Z; Ahmad, FJ; Talegaonkar, S  
  选自 期刊  Expert Opinion on Therapeutic Patents;  卷期  2011年21-4;  页码  561-576  
  关联知识点  
 

[摘要]Areas covered: This review explores the investigations on the feasibility and applicability of various classes of P-gp inhibitors as described in recent patents for enhanced drug delivery. Expert opinion: Several candidates presently under development look promising as P-gp inhibitors, e.g., tariquidar and elacridar. Pharmaceutical excipients currently constitute the most promising class of P-gp inhibitors and are considered safe and pharmaceutically acceptable for use in formulations. In addition, lipid-based excipients and thiolated polymers play an active role in affecting P-gp-mediated transport not only by altering the membrane fluidity or ATPase activity but by down regulating P-gp expression. An additional overture such as the prodrug derivatization of P-gp substrates is a feasible approach to bypass P-gp-mediated efflux.

 
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