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      Development of Liposome containing sodium deoxycholate to enhance oral bioavailability of itraconazole

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          Abstract

          The aim of this study was to enhance oral bioavailability of itraconazole (ITZ) by developing Liposome containing sodium deoxycholate (ITZ-Lip-NaDC). The liposome, consisting of egg yolk lecithin and sodium deoxycholate, was prepared by thin-film dispersion method. Differential Scanning Calorimetry (DSC) results indicated an amorphous state in the liposome. The physicochemical characteristics including particle size, morphology, entrapment efficiency, dissolution properties were also investigated. The performance of single-pass intestinal infusion exhibited that the transport order of intestinal segment was jejunum, duodenum, colon and ileum, and that all the segments participated in the absorption of ITZ in intestinal tract. The bioavailability study in rats showed that the AUC 0-72 of the liposome was nearly 1.67-fold higher than that of commercial capsules (SPORANOX) in terms of oral administration, and the RSD of AUC 0-72 of ITZ-Lip-NaDC was also decreased. Our results indicated that ITZ-Lip-NaDC liposome was facilitated to improve dissolution efficiency, augment transmembrane absorption, and then enhance the oral bioavailability of ITZ, successfully.

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          Prodrug-based nanoparticulate drug delivery strategies for cancer therapy.

          Cong Luo, Jin Sun, Bingjun Sun … (2014)
          Despite the rapid developments in nanotechnology and biomaterials, the efficient delivery of chemotherapeutic agents is still challenging. Prodrug-based nanoassemblies have many advantages as a potent platform for anticancer drug delivery, such as improved drug availability, high drug loading efficiency, resistance to recrystallization upon encapsulation, and spatially and temporally controllable drug release. In this review, we discuss prodrug-based nanocarriers for cancer therapy, including nanosystems based on polymer-drug conjugates, self-assembling small molecular weight prodrugs and prodrug-encapsulated nanoparticles (NPs). In addition, we discuss new trends in the field of prodrug-based nanoassemblies that enhance the delivery efficiency of anticancer drugs, with special emphasis on smart stimuli-triggered drug release, hybrid nanoassemblies, and combination drug therapy.
          Article 0 comments Cited 93 times – based on 0 reviews     Review now
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            Enhanced oral bioavailability of cyclosporine A by liposomes containing a bile salt

            Peipei Guan, Qiao-Yi Lu, Jianping Qi … (2011)
            The main purpose of this study was to evaluate liposomes containing a bile salt, sodium deoxycholate (SDC), as oral drug delivery systems to enhance the oral bioavailability of the poorly water-soluble and poorly permeable drug, cyclosporine A (CyA). Liposomes composed of soybean phosphatidylcholine (SPC) and SDC were prepared by a thin-film dispersion method followed by homogenization. Several properties of the liposomes including particle size, polydispersity index, and entrapment efficiency were characterized. The in vitro release of CyA from these liposomes was less than 5% at 12 hours as measured by a dynamic dialysis method. The pharmacokinetic results in rats showed improved absorption of CyA in SPC/SDC liposomes, compared with CyA-loaded conventional SPC/cholesterol (Chol) liposomes and microemulsion-based Sandimmune Neoral®. The relative oral bioavailability of CyA-loaded SPC/SDC and SPC/Chol liposomes was 120.3% and 98.6%, respectively, with Sandimmun Neoral as the reference. The enhanced bioavailability of CyA was probably due to facilitated absorption by the liposomes containing SDC rather than improved release rate.
            Article 0 comments Cited 44 times – based on 0 reviews     Review now
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              Stealth CD44-targeted hyaluronic acid supramolecular nanoassemblies for doxorubicin delivery: probing the effect of uncovalent pegylation degree on cellular uptake and blood long circulation.

              Yuhai Liu, Jin Sun, Cong Luo … (2015)
              Stealth active targeting nanoparticles (NPs) usually include two types of ligand sites: ligand anchored on distal ends of the polyethylene glycol (PEG) and ligand buried under pegylated layer. The latter typical case is hyaluronic acid (HA)-based NPs; however, there is little information available for the latter NPs about effect of the optimal density of surface PEG coating on the blood circulation time, cellular uptake and in vivo anticancer activity. Thus, in this study, in order to optimize the anticancer effects of HA-based NPs, we focus on how uncovalent pegylation degree modulates blood circulation time and cellular uptake of HA-based NPs. We firstly designed a new double-hydrophilic copolymer by conjugating HP-β-cyclodextrin with HA, and this carrier was further pegylated with adamantyl-peg (ADA-PEG) to form inclusion complex HA-HPCD/ADA-PEG, termed as HCPs. The supramolecular nanoassemblies were fabricated by host-guest and polar interactions between HCPs and doxorubicin (Dox), with vitamin E succinate (VES) being a nanobridge. Despite the active recognition between HA and CD44 receptor, the cellular uptake and targeting efficiency of HA-NPs decreased with the increasing peg density, demonstrating HA was partly buried by high density peg coating. However, the high density of peg coating was beneficial to long circulation time, tumor biodistribution and anticancer activity in vivo. NPs with 5% peg coating had the optimal cellular targeting efficiency in vitro and anticancer effects in vivo. The findings suggest that balancing long circulation property and cellular uptake is important to achieve the optimal antitumor efficacy for pegylated HA-based NPs, and that PEG coating densities cannot be extended beyond a certain density for shielding effect without compromising the efficacy of hyaluronic acid targeted delivery.
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                Author and article information

                Contributors
                Yinghua Sun
                Jin Sun
                Journal
                Journal ID (nlm-ta): Asian J Pharm Sci
                Journal ID (iso-abbrev): Asian J Pharm Sci
                Title: Asian Journal of Pharmaceutical Sciences
                Publisher: Shenyang Pharmaceutical University
                ISSN (Print): 1818-0876
                ISSN (Electronic): 2221-285X
                Publication date PMC-release: 04 August 2016
                Publication date (Print): March 2017
                Publication date (Electronic): 04 August 2016
                Volume: 12
                Issue: 2
                Pages: 157-164
                Affiliations
                [a ]School of Pharmacy, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, China
                [b ]Suihua No. 1 hospital, Beilin Road, Heilongjiang 152000, China
                [c ]School of further education, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, China
                [d ]Municipal Key Laboratory of Biopharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, China
                Author notes
                [* ]Corresponding author. School of Pharmacy, Shenyang Pharmaceutical University, No. 103 Wenhua Road, Shenyang 110016, China. Fax: +86 24 23986325. sunyinghua77@ 123456aliyun.com
                [** ]Corresponding author. School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China. Fax: +86 24 23986325. sunjin66@ 12345621cn.com
                Article
                Publisher ID: S1818-0876(16)30056-3
                DOI: 10.1016/j.ajps.2016.05.006
                PMC ID: 7032120
                PubMed ID: 32104325
                SO-VID: 959129ef-ebd0-47d9-aab2-66ea0c9e6e89
                Copyright © © 2017 Shenyang Pharmaceutical University. Production and hosting by Elsevier B.V.
                License:

                This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

                History
                Date received : 23 March 2016
                Date revision received : 7 May 2016
                Date accepted : 13 May 2016
                Categories
                Subject: Original Research Article

                Keywords: itraconazole,itz-lip-nadc,dissolution,intestinal infusion,oral bioavailability
                Data availability:
                Keywords: itraconazole, itz-lip-nadc, dissolution, intestinal infusion, oral bioavailability

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