Oramucosal delivery of LHRH: pharmacokinetic studies of controlled and enhanced transmucosal permeation

Pharmaceutical Development and Technology
S NakaneY W Chien

Abstract

Several transmucosal therapeutic systems (TmTs) were developed to study the enhanced/controlled delivery of luteinizing hormone-releasing hormone (LHRH) through oral mucosae for prolonged periods. TmTs is a track field-shaped bilayer mucoadhesive device consisting of fast-release and sustained-release layers. In vivo evaluations were performed in beagle dogs, and pharmacokinetic profiles were monitored to characterize the transmucosal permeation kinetics of LHRH delivered by the various TmTs formulations containing a stabilizer, cetylpyridinium chloride, and a permeation enhancer, such as bile salts, to enhance the stability and permeability of LHRH. The plasma LHRH concentrations were observed to reach the plateau level within 30 min and were maintained for 2 hr following application of TmTs, in contrast to a rapid elimination profile observed after IV administration. Addition of 5% bile salt into the fast-release layer was observed to produce an enhancement in the absorption rate, higher plateau plasma levels, and greater systemic bioavailability. Addition of pH modifiers was noted to affect the bile salt enhanced transmucosal delivery of LHRH. To prolong the plasma LHRH level, several loading doses of LHRH were incorporated ...Continue Reading

References

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Citations

Mar 1, 2014·Drug Development and Industrial Pharmacy·Flavia Laffleur
Aug 23, 2008·Drug Development and Industrial Pharmacy·G S AsaneY Madhusudan Rao
Apr 20, 2012·Expert Opinion on Drug Delivery·Nookala Venkala Satheesh MadhavRuchi B Semwal
Oct 9, 2007·Journal of Pharmaceutical Sciences·Rajesh SinghJames W Lillard
Jul 2, 2014·Journal of Controlled Release : Official Journal of the Controlled Release Society·Ronald A Siegel
Jul 10, 2012·Oral Surgery, Oral Medicine, Oral Pathology and Oral Radiology·Carlo PaderniGiuseppina Campisi
Dec 3, 2014·Journal of Controlled Release : Official Journal of the Controlled Release Society·Amardeep S Bhalla, Ronald A Siegel
Aug 30, 2014·Pharmaceutical Research·Thiago CaonJoseph A Nicolazzo
Jun 18, 2016·Journal of Pharmaceutical Sciences·Liang JinJoseph A Nicolazzo
Feb 19, 2004·Archives of Pharmacal Research·Su-Yun LyuWon-Bong Park
Nov 16, 2002·Archives of Pharmacal Research·Hye J Lee
Dec 2, 2006·European Journal of Drug Metabolism and Pharmacokinetics·M MikovS Kevresan
Oct 9, 2003·Clinical Pharmacokinetics·Stanley S Davis, Lisbeth Illum

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