Abstract：
:The objective of this study was to investigate the in vitro cytotoxicity and in vivo anticancer efficacy of redox-responsive microbeads containing thiolated pectin-doxorubicin (DOX) conjugate. Oral microbeads were coated with an enteric polymer to protect the drug from release in the upper gastrointestinal (GI) tract and allow redox-triggered drug release in the colon. Morphology, particle size, drug content, and in vitro drug release behavior of the microbeads were characterized; in vitro cytotoxicity was tested on mouse colon carcinoma, human colorectal adenocarcinoma, and human bone osteosarcoma cell lines. In vivo anticancer efficacy of coated microbeads was examined in BALB/c mice with murine colon carcinoma. These coated microbeads significantly inhibited the growth of all cell lines. The in vivo study confirmed delivery of DOX to the colorectal tumor site, redox-responsiveness, and anticancer efficacy of coated microbeads. Coated microbeads also effectively inhibited primary tumor growth and suppressed tumor metastases without gross toxicity to the non-target tissue. No noticeable damage was found in mouse GI tissues, indicating lack of DOX toxicity. These novel coated microbeads containing thiolated pectin-DOX conjugate may be a promising vehicle for targeted clinical delivery of DOX to the colorectal cancer site by oral administration.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Cheewatanakornkool K,Niratisai S,Dass CR,Sriamornsak Pdoi
10.1016/j.ijpharm.2018.04.052subject
Has Abstractpub_date
2018-07-10 00:00:00pages
1-9issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(18)30280-1journal_volume
545pub_type
杂志文章abstract：OBJECTIVES:The development of inhaled products to treat or to prevent lung infection is a very active research field in drug delivery. The pulmonary route is extremely attractive but very challenging. This paper reports the study of excipient, capsule brand and device influence on the aerodynamic behavior of dry powder...
journal_title：International journal of pharmaceutics
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abstract：:Public engagement in medication management has become more and more important in promoting population health. A public engagement workshop attended by 78 members of the geriatric community, family carers as well as professionals from academic research, industry and regulatory agencies entitled 'How to improve medicine...
journal_title：International journal of pharmaceutics
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doi：10.1016/j.ijpharm.2013.11.024
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abstract：:Efficacy of anticancer drug is limited by the severe adverse effects induced by drug; therefore the crux is in designing delivery systems targeted only to cancer cells. Toward this objectives, we propose, synthesis of poly(ethylene glycol) (PEG)-doxorubicin (DOX) prodrug conjugates consisting N-acetyl glucosamine (NAG...
journal_title：International journal of pharmaceutics
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abstract：:Low dose micro-tablets with acceptable quality attributes, specifically content uniformity (CU), would not only enhance the dose flexibility in the clinic, but also decrease excipient burden in pediatric population. Considering the CU challenges associated with directly compressed low dose micro-tablets, in this study...
journal_title：International journal of pharmaceutics
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更新日期：2020-09-25 00:00:00
abstract：:The purpose of this study was to produce salbutamol sulfate (SS) as a model anti-asthmatic drug using high-gravity controlled precipitation (HGCP) through antisolvent crystallisation. An aqueous solution of SS was passed through a HGCP reactor with isopropanol as antisolvent to induce precipitation. Spray drying was e...
journal_title：International journal of pharmaceutics
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abstract：:Gamma-oryzanol, a phytosteryl ferulate mixture extracted from rice bran oil, has a wide spectrum of biological activities; in particular, it has antioxidant properties and is often used in cosmetic formulations as a sunscreen. The first objective of the present investigation was to elucidate the molecular mechanism(s)...
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abstract：:Diabetic foot infections are the most common complications requiring hospitalisation of patients with diabetes. They often result in amputation to extremities and are associated with high morbi-mortality rates, especially when bone is infected. Treatment of these complications is based on surgical procedures, nursing ...
journal_title：International journal of pharmaceutics
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abstract：:A new chemical entity (NCE) was evaluated in the Clickhaler (Innovata Biomed Ltd.) dry powder inhaler, a reservoir-based multidose delivery system. The standard device metering system was modified to handle higher doses (nominally 20 mm(3) of lactose based blend). The micronized drug was formulated at 12.5% w/w in lac...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(02)00106-0
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abstract：:A series of thermoresponsive-co-biodegradable polymers, containing varying molar ratios of N-isopropylacrylamide (NIPA) and poly-lactic acid diacrylate macromer (PLAM) were prepared and characterised. Chemical structures were confirmed by nuclear magnetic resonance (NMR) and Fourier transform infrared (FTIR). The hydr...
journal_title：International journal of pharmaceutics
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.11.034
更新日期：2015-01-15 00:00:00
abstract：:Multiple sclerosis (MS) is the most common demyelinating disease. Despite the historical use of interferon-beta (IFN-β) for the treatment of patients with MS, concerns exist regarding the side effects of IFN-β. In this study, we designed a series of novel IFN-β fusion proteins containing galectin-9 (gal-9), which exer...
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pub_type： 杂志文章
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更新日期：2018-01-30 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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更新日期：2009-06-22 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.11.048
更新日期：2019-01-30 00:00:00
abstract：:An aerosol system is described for the generation and delivery of measured doses of monodisperse therapeutic drug particles to the human lungs. The system comprises a spinning top aerosol generator (STAG), aerosol chamber and inhalation control unit. Monodisperse aerosols allow drug particle size effects to be studied...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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更新日期：2003-03-26 00:00:00
abstract：:To reduce systemic bleeding risks during anticoagulant treatment, a new concept named "precise anticoagulation" was proposed to localize the effects of anticoagulants via the targeted delivery of prodrugs to the coagulation site. In this study, the fusion protein Annexin V-hirudin 3-ABD (hAvHA) was constructed to achi...
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更新日期：2020-09-10 00:00:00
abstract：:Currently, the compressed tablet and its oral administration is the most popular drug delivery modality in medicine. The accurate porosity and tensile strength characterization of a tablet design is vital for predicting its performance such as disintegration, dissolution, and drug-release efficiency upon administratio...
journal_title：International journal of pharmaceutics
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abstract：:The objective of this study was to prepare Herceptin (HCT)-functionalized paclitaxel nanocrystals and evaluated their cell-specific interactions, cellular accumulation, and growth inhibition in HER2-positve breast cancer cells as a tumor-targeted delivery module. Paclitaxel (PTX) was fabricated in the form of nanocrys...
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更新日期：2018-09-05 00:00:00
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pub_type： 杂志文章
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更新日期：2006-02-17 00:00:00
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更新日期：2010-12-15 00:00:00
abstract：:The systemic administration of methotrexate (MTX), a commonly used, antineoplastic drug which is also used in cutaneous disorders, is primarily associated with prolonged retention in the body and consequently with side effects. Innovative drug delivery techniques and alternative administration routes would therefore c...
journal_title：International journal of pharmaceutics
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更新日期：2017-09-15 00:00:00
abstract：:Subcutaneous vaccination of C57bl/6 mice with irradiated B16 melanoma cells supplemented with liposomal interleukin-2 (IL2) or murine interferon-gamma (mIFNgamma), resulted in systemic protection in 50% of the animals, against a subsequent tumor cell challenge in a dose dependent manner. The protective efficacy was co...
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更新日期：1999-06-10 00:00:00
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更新日期：2021-01-21 00:00:00
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abstract：:The present study puts forward a miniaturized high-throughput platform to understand influence of excipient selection and processing on the stability of a given drug compound. Four model drugs (sodium naproxen, theophylline, amlodipine besylate and nitrofurantoin) and ten different excipients were selected. Binary phy...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.08.025
更新日期：2013-08-30 00:00:00
abstract：:The maximum fluxes of a series of alkyloxycarbonyloxymethyl (AOCOM) ethers of acetaminophen (APAP) through hairless mouse skin from isopropyl myristate, IPM (J(MMIPM)) were measured. The J(MMIPM), solubilities in IPM (S(IPM)), water (S(AQ)) and pH 4.0 buffer (S4.0) and molecular weights MW were then fitted to the Robe...
journal_title：International journal of pharmaceutics
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doi：10.1016/j.ijpharm.2008.12.020
更新日期：2009-04-17 00:00:00
