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Pharmaceuticals 2018, 11(1), 9; doi:10.3390/ph11010009

Improved Intranasal Retentivity and Transnasal Absorption Enhancement by PEGylated Poly-l-ornithine

Faculty of Pharmaceutical Sciences, Josai University, 1-1 Keyakidai, Sakado, Saitama 350-0295, Japan
Laboratory of Drug Metabolism and Pharmacokinetics, Showa Pharmaceutical University, 3-3165 Higashi-tamagawa Gakuen, Machida, Tokyo 194-8543, Japan
Author to whom correspondence should be addressed.
Received: 28 October 2017 / Revised: 17 January 2018 / Accepted: 19 January 2018 / Published: 25 January 2018
(This article belongs to the Special Issue Polyethylene Glycol (PEG) and PEGylation in Pharmacy)
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We reported that the introduction of polyethylene glycol (PEG) to poly-l-ornithine (PLO), which is an homopolymeric basic amino acid having absorption-enhancement ability, prolonged retention time in an in vitro inclined plate test, probably due to an increase in viscosity caused by PEGylation. The aim of the present study is to investigate whether the introduction of PEG chains to PLO improves intranasal retention and transnasal absorption in vivo. We performed intranasal administration experiments using PLO and PEG-PLO with a model drug, fluorescein isothiocyanate dextran (FD-4), in rats under closed and open systems. In the open system, transition of plasma FD-4 concentration after co-administration with unmodified PLO was low, and the area under the plasma concentration-time curve (AUC) decreased to about 60% of that in the closed system. In contrast, the AUC after co-administration with PEG-PLO in the open system was about 90% of that in the closed system, and the transition of plasma FD-4 concentration and FD-4 absorption profile were similar to those of the closed system. These findings indicate that introducing PEG chains to homopolymeric basic amino acids (HPBAAs) is a very useful method for developing a functional absorption enhancer that can exhibit an efficient in vivo absorption-enhancing effect. View Full-Text
Keywords: poly-l-ornithine (PLO); polyethylene glycol (PEG); absorption enhancer; intranasal administration; retentivity poly-l-ornithine (PLO); polyethylene glycol (PEG); absorption enhancer; intranasal administration; retentivity

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Kamiya, Y.; Yamaki, T.; Omori, S.; Uchida, M.; Ohtake, K.; Kimura, M.; Yamazaki, H.; Natsume, H. Improved Intranasal Retentivity and Transnasal Absorption Enhancement by PEGylated Poly-l-ornithine. Pharmaceuticals 2018, 11, 9.

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