Liposomes for Enhanced Bioavailability of Water-Insoluble Drugs: In Vivo Evidence and Recent Approaches

It has been known that a considerable number of drugs in clinical use or under development are water-insoluble drugs with poor bioavailability (BA). The liposomal delivery system has drawn attention as one of the noteworthy approaches to increase dissolution and subsequently absorption in the gastro...

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Main Author: Mi-Kyung Lee
Format: Article
Language:English
Published: MDPI AG 2020-03-01
Series:Pharmaceutics
Subjects:
Online Access:https://www.mdpi.com/1999-4923/12/3/264
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author Mi-Kyung Lee
author_facet Mi-Kyung Lee
author_sort Mi-Kyung Lee
collection DOAJ
description It has been known that a considerable number of drugs in clinical use or under development are water-insoluble drugs with poor bioavailability (BA). The liposomal delivery system has drawn attention as one of the noteworthy approaches to increase dissolution and subsequently absorption in the gastrointestinal (GI) tract because of its biocompatibility and ability to encapsulate hydrophobic molecules in the lipid domain. However, there have been several drawbacks, such as structural instability in the GI tract and poor permeability across intestinal epithelia because of its relatively large size. In addition, there have been no liposomal formulations approved for oral use to date, despite the success of parenteral liposomes. Nevertheless, liposomal oral delivery has resurged with the rapid increase of published studies in the last decade. However, it is discouraging that most of this research has been in vitro studies only and there have not been many water-insoluble drugs with in vivo data. The present review focused on the in vivo evidence for the improved BA of water-insoluble drugs using liposomes to resolve doubts raised concerning liposomal oral delivery and attempted to provide insight by highlighting the approaches used for in vivo achievements.
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spelling doaj.art-3501bd33b4f84e7bb3500a9fc37c1bdb2022-12-22T04:01:37ZengMDPI AGPharmaceutics1999-49232020-03-0112326410.3390/pharmaceutics12030264pharmaceutics12030264Liposomes for Enhanced Bioavailability of Water-Insoluble Drugs: In Vivo Evidence and Recent ApproachesMi-Kyung Lee0Department of Pharmaceutical Sciences, Woosuk University, Jeonbuk 55338, KoreaIt has been known that a considerable number of drugs in clinical use or under development are water-insoluble drugs with poor bioavailability (BA). The liposomal delivery system has drawn attention as one of the noteworthy approaches to increase dissolution and subsequently absorption in the gastrointestinal (GI) tract because of its biocompatibility and ability to encapsulate hydrophobic molecules in the lipid domain. However, there have been several drawbacks, such as structural instability in the GI tract and poor permeability across intestinal epithelia because of its relatively large size. In addition, there have been no liposomal formulations approved for oral use to date, despite the success of parenteral liposomes. Nevertheless, liposomal oral delivery has resurged with the rapid increase of published studies in the last decade. However, it is discouraging that most of this research has been in vitro studies only and there have not been many water-insoluble drugs with in vivo data. The present review focused on the in vivo evidence for the improved BA of water-insoluble drugs using liposomes to resolve doubts raised concerning liposomal oral delivery and attempted to provide insight by highlighting the approaches used for in vivo achievements.https://www.mdpi.com/1999-4923/12/3/264liposomesoralabsorptionwater-insoluble drugsbioavailability
spellingShingle Mi-Kyung Lee
Liposomes for Enhanced Bioavailability of Water-Insoluble Drugs: In Vivo Evidence and Recent Approaches
Pharmaceutics
liposomes
oral
absorption
water-insoluble drugs
bioavailability
title Liposomes for Enhanced Bioavailability of Water-Insoluble Drugs: In Vivo Evidence and Recent Approaches
title_full Liposomes for Enhanced Bioavailability of Water-Insoluble Drugs: In Vivo Evidence and Recent Approaches
title_fullStr Liposomes for Enhanced Bioavailability of Water-Insoluble Drugs: In Vivo Evidence and Recent Approaches
title_full_unstemmed Liposomes for Enhanced Bioavailability of Water-Insoluble Drugs: In Vivo Evidence and Recent Approaches
title_short Liposomes for Enhanced Bioavailability of Water-Insoluble Drugs: In Vivo Evidence and Recent Approaches
title_sort liposomes for enhanced bioavailability of water insoluble drugs in vivo evidence and recent approaches
topic liposomes
oral
absorption
water-insoluble drugs
bioavailability
url https://www.mdpi.com/1999-4923/12/3/264
work_keys_str_mv AT mikyunglee liposomesforenhancedbioavailabilityofwaterinsolubledrugsinvivoevidenceandrecentapproaches