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        Zwitterionic mesoporous nanoparticles with a bioresponsive gatekeeper for cancer therapy

        Khatoon, S.,Han, H.S.,Lee, M.,Lee, H.,Jung, D.W.,Thambi, T.,Ikram, M.,Kang, Y.M.,Yi, G.R.,Park, J.H. Elsevier BV 2016 ACTA BIOMATERIALIA Vol.40 No.-

        To enhance cellular uptake and site-specific drug release in the tumor microenvironment, zwitterionic mesoporous silica nanoparticles (Z-MSN) were prepared by introducing a bioresponsive gatekeeper composed of negatively charged carboxylic groups and positively charged quaternary amine groups. When these Z-MSN encountered a mildly acidic environment, their surface charge readily switched from negative to positive by cleavage of an acid-labile maleic amide linkage, thus allowing for effective cellular uptake into tumor tissue. Doxorubicin (DOX) encapsulated in Z-MSN was not significantly released in physiological conditions (pH 7.4), whereas the release rate of DOX remarkably increased in mildly acidic conditions through disintegration of the gatekeeper. The antitumor efficacy of DOX-loaded Z-MSN (DOX-Z-MSN) was evaluated after their systemic administration to tumor-bearing mice. Compared to free DOX and DOX-loaded MSN without the gatekeeper, DOX-Z-MSN exhibited much higher antitumor efficacy in vivo. Overall, these results demonstrated that the hydrophilic negative surface of Z-MSN, with their closed gate, allowed for their effective accumulation in tumor tissue after systemic administration, and that their charge-swapping and gate-opening in the tumor environment enhanced their cellular uptake and drug release rate simultaneously, implying a highly promising potential for development of Z-MSN as a drug carrier for cancer therapy. Statement of Significance: In an attempt to address the issues of enhanced cellular uptake and site-specific drug release of nanoparticles, we herein report on zwitterionic MSN (Z-MSN) with a pH-responsive gatekeeper which can be internalized into cancer cells via switching their surface charge from negative, in physiological conditions, to positive, in the tumor microenvironment. We hypothesized that the hydrophilic negative surface of Z-MSN with a closed gate allows for their accumulation into tumor tissue after systemic administration, whereas their charge-swapping and gate-opening in the tumor environment enhance cellular uptake and drug release rate simultaneously. Overall, Z-MSN constitute a promising drug delivery carrier for cancer therapy.

      • KCI등재후보

        Pharmacognostical Evaluation of Leucas aspera Link.

        Vartika Rai,Manisha Agarwal,A.K. Agnihotri,S. Khatoon,A.K.S. Rawat,S. Mehrotra 한국생약학회 2005 Natural Product Sciences Vol.11 No.2

        Leucas aspera Link. (Lamiaceae) is an important medicinal plant in indigenous systems of medicinecomunities find diverse medicinal properties. It is used as antipyretic, stimulant, expectorant and diaphoreticdrug. The present communication deals with the detailed pharmacognostical evaluation of whole plant of L.aspera collected from five different geographical zones of the country-Uttar Pradesh, Orissa, Karnataka, WestBengal and Gujarat. The botanical characters and TLC fingerprint profile of all the samples were quite similar butsome variations were observed in physicochemical parameters. However, some microscopical characters and TLCprofile can be used as diagnostic characters for identification of , for example amphistomachic leavesand two types of trichomes-abundant, non glandular, uniseriate, 1-3 celled and few glandular, 2-5 celled stalk withrounded tip. Presence of some components at Rfs-0.56, 0.65 and 0.76 under UV 366 and at Rfs-0.31, 0.43, 0.60,0.76 and 0.82 under visible light after derivetization in TLC profile may also be used as diagnostic character.

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      • KCI등재후보
      • KCI등재

        Accessibility and site suitability for healthcare services using GISbased hybrid decision-making approach: a study in Murshidabad, India

        Parvin Farhana,Ali Sk Ajim,Hashmi S. Najmul Islam,Khatoon Aaisha 대한공간정보학회 2021 Spatial Information Research Vol.29 No.1

        Healthcare accessibility and site suitability analysis is an elongated and complex task that requires evaluation of different decision factors. The main objective of the present study was to develop a hybrid decisionmaking approach with geographic information systems to integrate spatial and non-spatial data to form a weighted result. This study involved three-tier analyses for assessing accessibility and selecting suitable sites for healthcare facilities, and analysing shortest-path network. The first tier of analysis stressed the spatial distance, density and proximity from existing healthcare to find more deprived and inaccessible areas in term of healthcare facilities. The result revealed that spatial discrepancy exists in the study area in term of access to healthcare facilities and for achieving equal healthcare access, it is essential to propose new plans. Thus, require finding suitable sites for put forward new healthcare service, which was highlighted in the second tier of analysis based on land use land cover, distancing to road and rail, proximity to residential areas, and weighted overlay of accessibility as decision factors. Finally, in the third tier of analysis, the most suitable site among the proposed healthcare was identified using the technique for order of preference by similarity to ideal solution. The road network analysis was also performed in this study to determine the shortest and fastest route from these healthcare facilities to connect with district medical hospital. The present study found some suitable sites throughout the district on inaccessible zones where people are deprived from better healthcare facilities. This attempt will highly helpful for preparing a spatial decision support system which assists the health authorities regarding the healthcare services in inaccessible, underprivileged, and rural areas.

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