The studies of N-Octyl-N-Arginine-Chitosan coated liposome as an oral delivery system of Cyclosporine A

Deng, Jin; Zhang, Zhenhai; Liu, Chunyan; Yin, Lifang; Zhou, Jianping; Lv, Huixia

doi:10.1111/jphp.12448

Cited by 31 publications

(10 citation statements)

References 18 publications

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“…Dialysis method was used to investigate the in vitro release pattern of BAI‐M. A total of 1 ml of BAI‐M or an equivalent amount of BAI crystal as control was added into dialysis bags (molecular weight cut‐off was 3500 g/mol; Green Bird Inc., Shanghai, China) . Freshly prepared 200 ml of release medium containing phosphate‐buffered saline (PBS, pH 7.4, 37°C) with 0.5% (w/v) Tween 80, and the whole process was under sink condition.…”

Section: Methodsmentioning

confidence: 99%

“…Dialysis method was used to investigate the in vitro release pattern of BAI-M. A total of 1 ml of BAI-M or an equivalent amount of BAI crystal as control was added into dialysis bags (molecular weight cut-off was 3500 g/mol; Green Bird Inc., Shanghai, China). [21] Freshly prepared 200 ml of release medium containing phosphate-buffered saline (PBS, pH 7.4, 37°C) with 0.5% (w/v) Tween 80, and the whole process was under sink condition. At predetermined time intervals (1, 2, 3, 6, 8, 10, 20, 30, 40 and 60 h after test), triplicate suspensions (0.5 ml) were withdrawn from the release medium and filtered through a 0.22-lm microporous membrane for analysis and replaced with the same volume of fresh medium.…”

Section: In Vitro Release Studymentioning

confidence: 99%

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Enhancing the oral bioavailability of baicalein via Solutol® HS15 and Poloxamer 188 mixed micelles system

Shen

Liu

Zhang

et al. 2019

Journal of Pharmacy and Pharmacology

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Objectives To increase the solubility of baicalein (BAI) by preparing BAI‐micelles (BAI‐M) with Solutol HS15 (HS15) and Poloxamer 188 (F68), thereby improving its oral bioavailability. Methods Baicalein micelles were prepared with HS15 and F68 by thin‐film dispersion method and optimized by central composite design (CCD) approach. Physicochemical, in vitro release, Caco‐2 cell transport and pharmacokinetic studies of BAI‐M were performed. Key findings The optimal formulation showed spherical shape by characterization of the transmission electron microscope with average small size (23.14 ± 1.46 nm) and high entrapment efficiency (92.78±0.98%) and drug loading (6.45±1.54%). The in vitro release study of BAI‐M showed a significantly sustained release pattern compared with free BAI. Caco‐2 cell transport study demonstrated that high permeability of BAI was achieved after loading it into micelles. Meanwhile, pharmacokinetics study of BAI‐M showed a 3.02‐fold increase in relative oral bioavailability compared with free BAI. Conclusions Based on our findings, we concluded that HS15 can be used as a carrier in this drug delivery system that includes F68, and BAI‐M has great potential in improving solubility and oral bioavailability.

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Section: Methodsmentioning

confidence: 99%

Section: In Vitro Release Studymentioning

confidence: 99%

Enhancing the oral bioavailability of baicalein via Solutol® HS15 and Poloxamer 188 mixed micelles system

Shen

Liu

Zhang

et al. 2019

Journal of Pharmacy and Pharmacology

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“…However, the TMC layer was covered by the CMCS layer because of cell rupture by TMC [38]. 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].…”

Section: Modification With Chitosan and Its Derivativesmentioning

confidence: 99%

“…Another study adopted N-octyl-N-arginine-chitosan (OACS), a derivative of chitosan, to evaluate permeability-enhancing ability by arginine-rich peptide and drug-loading capacity by the amphiphilic polymers to modify the liposomes consisted with SPC and CH (20:1) [41]. The OACS-modified liposomes (using OACS with 10% of octyl substitution and 10% of arginine substitution) increased oral BA of cyclosporine A by 3.2-fold compared to the free drug suspension, while unmodified liposomes did so by 1.7-fold.…”

Section: Cyclosporine Amentioning

confidence: 99%

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

Lee

2020

Pharmaceutics

189

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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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“…Chitosan, a natural polysaccharide, has been widely explored for drug delivery because of its biocompatibility, absorption enhancement and active functional groups for chemical modifications [16][17][18]. In this study, a novel amphiphilic derivatized polymer, N-(4-methylimidazole)-hydroxyethyl-chitosan (MHC), which can spontaneously form nanometric micelles in water and act as an excellent carrier with drug-protective properties and capability of controlled release, was used [19].…”

Section: Introductionmentioning

confidence: 99%

Promising positive liver targeting delivery system based on arabinogalactan-anchored polymeric micelles of norcantharidin

Zhang

Yang

Hou

et al. 2018

Artificial Cells, Nanomedicine, and Biotechnology

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2018) Promising positive liver targeting delivery system based on arabinogalactananchored polymeric micelles of norcantharidin, Artificial Cells, Nanomedicine, and Biotechnology, 46:sup3, S630-S640, ABSTRACT Liver cancer is the third most common cause of global cancer-related deaths. This study focused on newly developed drug delivery systems with hepatocyte asialoglycoprotein receptor binding targeting the liver. Although norcantharidin (NCTD) is effective in primary liver cancer treatment, its toxicity in the urinary system remains. Positive liver-targeting effect could be achieved by preparing polymer micelles by arabinogalactan on the surface of N-(4-methylimidazole)-hydroxyethyl-chitosan (MHC).HepG2 cells were used to analyze the cytotoxicity, invasion, apoptosis and uptake of NCTD-loaded micelles. The in vivo antitumor efficacy of NCTD-M was evaluated using tumor-bearing nude mice. Successful preparation of NCTD-M was shown. In vivo imaging showed that micelles significantly increased positive liver drug targeting. Laser confocal microscopy showed increased cellular uptake of micelles. NCTD-M also enhanced cell invasion and the proportion of apoptotic cells. Compared with the other groups, the micelles showed better antitumor effects in vivo. Therefore, the positive liver-targeting NCTD-M, which can enhance antitumor efficacy and reduce toxicity, could be a promising and effective therapeutic agent for liver cancer treatment.

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The studies of N-Octyl-N-Arginine-Chitosan coated liposome as an oral delivery system of Cyclosporine A

Abstract: Therefore, OACS coated liposomes can be an effective strategy to promote drug's absorption and further reduce the anaphylactic reaction of abundant surfactants in commercial preparations.

Cited by 31 publications

References 18 publications

Enhancing the oral bioavailability of baicalein via Solutol® HS15 and Poloxamer 188 mixed micelles system

Enhancing the oral bioavailability of baicalein via Solutol® HS15 and Poloxamer 188 mixed micelles system

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

Promising positive liver targeting delivery system based on arabinogalactan-anchored polymeric micelles of norcantharidin

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