Enhanced oral absorption of sorafenib via the layer-by-layer deposition of a pH-sensitive polymer and glycol chitosan on the liposome

Zhao, Mingguo; Lee, Sang Hoon; Song, Jae Geun; Kim, Hyeon Young; Han, Hyo-Kyung

doi:10.1016/j.ijpharm.2018.04.020

Cited by 59 publications

(30 citation statements)

References 33 publications

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“…The surface of liposomes can be coated with pH-dependent polymers to avoid the destabilization of liposomes in acidic conditions and also with ligands to improve the site-specificity. For example, Zhao et al [34] developed colon-targeted liposomal formulations for sorafenib by coating the surface of anionic liposomes with glycol chitosan and pH-dependent Eudragit ® S100. These liposomes showed high stability at acidic and neutral pHs with minimal drug leakage, which enhanced the systemic exposure of sorafenib in rats [34].…”

Section: Lipid-based Formulationsmentioning

confidence: 99%

Strategic Approaches for Colon Targeted Drug Delivery: An Overview of Recent Advancements

et al. 2020

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Colon targeted drug delivery systems have gained a great deal of attention as potential carriers for the local treatment of colonic diseases with reduced systemic side effects and also for the enhanced oral delivery of various therapeutics vulnerable to acidic and enzymatic degradation in the upper gastrointestinal tract. In recent years, the global pharmaceutical market for biologics has grown, and increasing demand for a more patient-friendly drug administration system highlights the importance of colonic drug delivery as a noninvasive delivery approach for macromolecules. Colon-targeted drug delivery systems for macromolecules can provide therapeutic benefits including better patient compliance (because they are pain-free and can be self-administered) and lower costs. Therefore, to achieve more efficient colonic drug delivery for local or systemic drug effects, various strategies have been explored including pH-dependent systems, enzyme-triggered systems, receptor-mediated systems, and magnetically-driven systems. In this review, recent advancements in various approaches for designing colon targeted drug delivery systems and their pharmaceutical applications are covered with a particular emphasis on formulation technologies.

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Section: Lipid-based Formulationsmentioning

confidence: 99%

Strategic Approaches for Colon Targeted Drug Delivery: An Overview of Recent Advancements

et al. 2020

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“…Therefore, effective strategies for improving oral absorption are urgently needed. Nanocarriers, such as liposomes, 1 nanoparticles, 2,3 nanocrystals, 4 and micelles, 5 have unique physicochemical properties to overcome intestinal epithelial barrier and have attracted more attention in improving the efficiency of oral drug delivery. 6 Nowadays, polymeric micelles (PMs) are promising vehicles to increase the oral absorption of hydrophobic drugs.…”

Section: Introductionmentioning

confidence: 99%

Apically targeted oral micelles exhibit highly efficient intestinal uptake and oral absorption

Wang¹,

Wang²,

Liu³

et al. 2018

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IntroductionPolymeric micelles (PMs) hold promise for improving solubility and oral absorption of poorly soluble drugs. Unfortunately, the oral absorption of PMs is also limited by intestinal epithelium. To improve the oral delivery efficiency of micelles, transporter-mediated micelles could enhance the transport efficiency across the epithelial barrier, and they have attracted more attention.MethodsPeptide transporter 1 (PepT1)-mediated micelles (Val-PMs/Phe-PMs) were designed by grafting valine (or phenylalanine) onto the surface of curcumin (Cur)-loaded-D-α-tocopheryl polyethylene glycol 1000 succinate micelles (TP-PMs). The oral absorption mechanism and oral bioavailability were further investigated in vitro and in vivo.ResultsThe cellular study showed that Val-PMs/Phe-PMs had a high PepT1 affinity, resulting in a higher drug uptake and transcellular transport than TP-PMs. In rats, Val-PMs/Phe-PMs exhibited higher intestinal accumulation in the apical side of the intestinal epithelium than TP-PMs, promoting drug diffusion across epithelial barrier. The oral bioavailability of Cur was significantly improved by Val-PMs/Phe-PMs, which was about 10.50- and 3.40-fold greater than that of Cur-Sol and TP-PMs, respectively.ConclusionPepT-1-mediated micelles, using PepT1 as a target on intestinal epithelium, have unique functions with intestine and prove promising for oral delivery of poorly water-soluble drugs.

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“…In the studies listed in Table 1, enteric coating was accomplished through a charge interaction between positively charged liposomes and negatively charged coating agents such as Eudragit S100 and L100. Enteric coating effect was prominent, showing 3.1-and 5.1-fold increases of BA for docetaxel and sorafenib, respectively, as shown in Table 1 [19,30,63]. In contrast, coating with CAP increased the BA of halofantrine only by 1.4-fold [63].…”

Section: Surface Modificationmentioning

confidence: 96%

“…The arginine derivative of chitosan, OACS, was also attempted to increase the permeation of the drug in the mucosal barrier [41]. Another chitosan derivative, GC, was newly introduced because it is water-soluble and cationic at physiological pH, while chitosan has a very low solubility above pH 6.5, with the loss of cationic charge [30,70]. Moreover, chitosan coating has been considered to increase the membrane integrity and physical stability of liposomes [71].…”

Section: Modification With Chitosan and Its Derivativesmentioning

confidence: 99%

“…In addition, large interpatient variations have been reported in the pharmacokinetics of sorafenib, which was supposed to result from slow dissolution in the GI tract [111]. Zhao et al tried to develop an improved delivery system to prolong the residence time in the colon to increase drug absorption using enteric-coated liposomes [30]. They prepared negatively charged liposomes composed with DPPC, DPPG, TPGS, CH and drug (8:1:2:4:1).…”

Section: Sorafenibmentioning

confidence: 99%

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

Lee

2020

Pharmaceutics

187

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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.Pharmaceutics 2020, 12, 264 2 of 30 However, there have been several drawbacks to be overcome, such as instability in the GI tract and poor permeability across the intestinal epithelia because of liposomes' relatively large size [8]. Moreover, it seemed that liposomal oral delivery was faltering during 1980s due to some disappointing results for insulin [9]. However, liposomal oral delivery resurged with a rapid increase in the number of papers published, as shown in Pubmed search results, mainly due to various advanced modification technologies, even though liposomal oral delivery-related papers account for only 5-6% of the total number of liposomes-related studies (Figure 1). In addition, there was an encouraging meta-analysis report in which phospholipid-based solid formulations were analyzed as being effective for BA enhancement [10]. Although liposomal delivery does not seem to achieve satisfactory improvement of oral BA for peptides and protein drugs yet, it looks more promising for oral delivery of hydrophobic drugs because liposomes can solubilize poorly water-soluble drugs, protect the drug from degradation in the GI tract and enhance permeability through the epithelial cell membrane, consequently increasing oral BA. However, most published papers performed in vitro studies only, thus lacking in vivo pharmacokinetic results. The present review focuses on the in vivo evidence for the improved BA of water-insoluble drugs and highlights the approaches used for in vivo achievements.

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Enhanced oral absorption of sorafenib via the layer-by-layer deposition of a pH-sensitive polymer and glycol chitosan on the liposome

Cited by 59 publications

References 33 publications

Strategic Approaches for Colon Targeted Drug Delivery: An Overview of Recent Advancements

Strategic Approaches for Colon Targeted Drug Delivery: An Overview of Recent Advancements

Apically targeted oral micelles exhibit highly efficient intestinal uptake and oral absorption

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

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