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      Preparation and Evaluation of Poly-Butylcyanoacrylate Nanoparticles for Oral Delivery of Thymopentin

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          Abstract

          Thymopentin (Tp5) was loaded in poly-butylcyanoacrylate (PBCA) nanoparticles (NP) in order to enhance the oral bioavailability of Tp5. PBCA-Tp5-NP was prepared by nanoprecipitation methods. Dialyzing membrane method was employed to examine the in vitro release of PBCA-Tp5-NP in PBS, and Tp5 samples in the release medium were detected by HPLC. The cell proliferation test ( 3H-thymidine) was conducted to verify the PBCA-Tp5-NP bioactivity in vitro. The pharmacodynamical studies were performed on preimmunoinhibited rats and in flow cytometer. The size and the entrapment efficiency of PBCA-Tp5-NP were 178 ± 39 nm and 92.21 ± 1.08%, respectively. In vitro release data show that less than 60% Tp5 was released from lyophilized PBCA-Tp5-NP while 80% Tp5 was released from the colloidal PBCA-Tp5-NPs in 48 h. The proliferation test showed that PBCA-Tp5-NP had the similar effect as Tp5. The in vivo data showed that oral PBCA-Tp5-NPs had similar function as what intravenous Tp5 did. The oral bioavailability of Tp5 could be enhanced by PBCA nanoparticles. PBCA-Tp5-NP had the property of sustained-release and the efficacy of Tp5 was not changed after formulation.

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          Biologically erodable microspheres as potential oral drug delivery systems.

          E Mathiowitz, G Carino, Polly S. Montgomery … (1997)
          Biologically adhesive delivery systems offer important advantages over conventional drug delivery systems. Here we show that engineered polymer microspheres made of biologically erodable polymers, which display strong adhesive interactions with gastrointestinal mucus and cellular linings, can traverse both the mucosal absorptive epithelium and the follicle-associated epithelium covering the lymphoid tissue of Peyer's patches. The polymers maintain contact with intestinal epithelium for extended periods of time and actually penetrate it, through and between cells. Thus, once loaded with compounds of pharmacological interest, the microspheres could be developed as delivery systems to transfer biologically active molecules to the circulation. We show that these microspheres increase the absorption of three model substances of widely different molecular size: dicumarol, insulin and plasmid DNA.
          Article 0 comments Cited 98 times – based on 0 reviews     Review now
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            Poly(d,l-lactide-co-glycolide)/montmorillonite nanoparticles for oral delivery of anticancer drugs.

            Yuancai Dong, Shen Feng (2005)
            This research developed a novel bioadhesive drug delivery system, poly(d,l-lactide-co-glycolide)/montmorillonite (PLGA/MMT) nanoparticles, for oral delivery of paclitaxel. Paclitaxel-loaded PLGA/MMT nanoparticles were prepared by the emulsion/solvent evaporation method. MMT was incorporated in the formulation as a matrix material component, which also plays the role of a co-emulsifier in the nanoparticle preparation process. Paclitaxel-loaded PLGA/MMT nanoparticles were found to be of spherical shape with a mean size of around 310 nm and polydispersity of less than 0.150. Adding MMT component to the matrix material appears to have little influence on the particles size and the drug encapsulation efficiency. The drug release pattern was found biphasic with an initial burst followed by a slow, sustained release, which was not remarkably affected by the MMT component. Cellular uptake of the fluorescent coumarin 6-loaded PLGA/MMT nanoparticles showed that MMT enhanced the cellular uptake efficiency of the pure PLGA nanoparticles by 57-177% for Caco-2 cells and 11-55% for HT-29 cells, which was dependent on the amount of MMT and the particle concentration in incubation. Such a novel formulation is expected to possess extended residence time in the gastrointestinal (GI) tract, which promotes oral delivery of paclitaxel.
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              Polysorbate-80 coating enhances uptake of polybutylcyanoacrylate (PBCA)-nanoparticles by human and bovine primary brain capillary endothelial cells.

              P Ramge, R E Unger, J B Oltrogge … (2000)
              Certain drugs such as dalargin, loperamide or tubocurarine are not transported across the blood-brain barrier (BBB) and therefore exhibit no effects on the central nervous system. However, effects on the central nervous system can be observed when these drugs are loaded onto polybutylcyanoacrylate (PBCA)-nanoparticles and coated with polysorbate 80. The mechanism by which these complexed nanoparticles cross the BBB and exhibit their effects has not been elucidated. Cultured microvessel brain endothelial cells of human and bovine origin were used as an in vitro model for the BBB to gain further insight into the mechanism of uptake of nanoparticles. With cells from these species we were able to show that polysorbate 80-coated nanoparticles were taken up by brain endothelial cells much more rapidly and in significantly higher amounts (20-fold) than uncoated nanoparticles. The process of uptake was followed by fluorescence and confocal laser scanning microscopy. The results demonstrate that the nanoparticles are taken up by cells and that this uptake occurs via an endocytotic mechanism.
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                Author and article information

                Contributors
                Zhi-Rong Zhang
                Journal
                Journal ID (nlm-ta): J Pharm Sci
                Journal ID (iso-abbrev): J Pharm Sci
                Title: Journal of Pharmaceutical Sciences
                Publisher: Elsevier
                ISSN (Print): 0022-3549
                ISSN (Electronic): 1520-6017
                Publication date PMC-release: 28 January 2016
                Publication date (Print): June 2008
                Publication date (Electronic): 28 January 2016
                Volume: 97
                Issue: 6
                Pages: 2250-2259
                Affiliations
                [1 ]University of Wyoming School of Pharmacy, Laramie, Wyoming 82071
                [2 ]Education Ministry Key Laboratory of Drug Targeting and Drug Delivery Systems, National Key Laboratory of Biotherapy, West-China School of Pharmacy, Sichuan University, Chengdu 610041, China
                Author notes
                [* ]Education Ministry Key Laboratory of Drug Targeting and Drug Delivery Systems, National Key Laboratory of Biotherapy, West-China School of Pharmacy, Sichuan University, Chengdu 610041, China Telephone: +86-28-85501566; Fax: +86-28-85456898 zrzzl@ 123456vip.sina.com
                Article
                Publisher ID: S0022-3549(16)32594-1
                DOI: 10.1002/jps.21148
                PMC ID: 7094308
                PubMed ID: 17853430
                SO-VID: 7b00b4b1-c214-4044-b4ca-c09a0b105059
                Copyright © © 2007 Wiley-Liss, Inc.
                License:

                Since January 2020 Elsevier has created a COVID-19 resource centre with free information in English and Mandarin on the novel coronavirus COVID-19. The COVID-19 resource centre is hosted on Elsevier Connect, the company's public news and information website. Elsevier hereby grants permission to make all its COVID-19-related research that is available on the COVID-19 resource centre - including this research content - immediately available in PubMed Central and other publicly funded repositories, such as the WHO COVID database with rights for unrestricted research re-use and analyses in any form or by any means with acknowledgement of the original source. These permissions are granted for free by Elsevier for as long as the COVID-19 resource centre remains active.

                History
                Date received : 7 December 2006
                Date revision received : 5 March 2007
                Date accepted : 3 July 2007
                Categories
                Subject: Article

                ScienceOpen disciplines: Pharmacology & Pharmaceutical medicine
                Keywords: thymopentin,oral drug delivery,bioavailability,pbca,nanoparticles
                Data availability:
                ScienceOpen disciplines: Pharmacology & Pharmaceutical medicine
                Keywords: thymopentin, oral drug delivery, bioavailability, pbca, nanoparticles

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