Nasal polysaccharides-glucose regulator microparticles: Optimization, tolerability and antidiabetic activity in rats

被引：22
作者：
Elmowafy, Enas [1 ]
Osman, Rihab [1 ]
El-Shamy, Abd El-Hameed A. [1 ]
Awad, Gehanne A. S. [1 ]
机构：
[1] Ain Shams Univ, Fac Pharm, Dept Pharmaceut & Ind Pharm, Cairo, Egypt
来源：
CARBOHYDRATE POLYMERS | 2014年 / 108卷
关键词：
Microparticles; Polysaccharides; Antidiabetic; Spray drying; Nasal powder; Insufflator; IN-VITRO; DELIVERY-SYSTEM; DRUG-DELIVERY; GELLAN GUM; REPAGLINIDE; CHITOSAN; MICROSPHERES; RELEASE; HYDROCHLORIDE; DEPOSITION;
D O I：
10.1016/j.carbpol.2014.02.064
中图分类号：
O69 [应用化学];
学科分类号：
081704 ;
摘要：
The aim of the present study was to load the post-prandial glucose regulator, repaglinide (REP), on spray dried mucoadhesive microparticles (MPs) comprising anionic polysaccharides. The formulation parameters of the polysaccharides-REP spray dried powders (SDP) namely, polysaccharide type and drug to polymer (D/P) ratio, were optimized for % release after 5 min (R%(5 min)) and time required for 80% release (T-80%). The suitability of the selected formulae for nasal application was evaluated by ex vivo mucoadhesion, in vitro cytocompatability and tolerability studies. A pharmacodynamic study in diabetic rats was conducted. Results showed that both polysaccharide type and amount greatly influenced the chosen responses. REP was highly incorporated in mucoadhesive MPs with proven safety on the rat nasal mucosa. The selected REP loaded powders exhibited a significant two to threefold increase in total decrease in blood glucose compared to the nasal and intravenous solutions. (C) 2014 Elsevier Ltd. All rights reserved.
引用
收藏
页码：257 / 265
页数：9
相关论文
共 41 条
[1]  
Abeeleh MA., 2009, European Journal of Scientific Research, V32, P398
[2]   Preparation of zolmitriptan-chitosan microparticles by spray drying for nasal delivery [J].
Alhalaweh, Amjad ;
Andersson, Staffan ;
Velaga, Sitaram P. .
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2009, 38 (03) :206-214
[3]   Preparation, characterization, in vitro drug release and biological studies of curcumin loaded dextran sulphate-chitosan nanoparticles [J].
Anitha, A. ;
Deepagan, V. G. ;
Rani, V. V. Divya ;
Menon, Deepthy ;
Nair, S. V. ;
Jayakumar, R. .
CARBOHYDRATE POLYMERS, 2011, 84 (03) :1158-1164
[4]   Synthesis and characterization of the inclusion complex between repaglinide and sulfobutylether-β-cyclodextrin (Captisol®) [J].
Arama, Corina ;
Nicolescu, Camelia ;
Nedelcu, Angela ;
Monciu, Crina-Maria .
JOURNAL OF INCLUSION PHENOMENA AND MACROCYCLIC CHEMISTRY, 2011, 70 (3-4) :421-428
[5]   Meglitinide analogues:: a review of clinical data focused on recent trials [J].
Blicklé, JF .
DIABETES & METABOLISM, 2006, 32 (02) :113-120
[6]   Chitosan and cyclodextrin in intranasal microemulsion for improved brain buspirone hydrochloride pharmacokinetics in rats [J].
Bshara, Hamza ;
Osman, Rihab ;
Mansour, Samar ;
El-Shamy, Abd El-Hameed A. .
CARBOHYDRATE POLYMERS, 2014, 99 :297-305
[7]   Particles and powders: Tools of innovation for non-invasive drug administration [J].
Buttini, Francesca ;
Colombo, Paolo ;
Rossi, Alessandra ;
Sonvico, Fabio ;
Colombo, Gaia .
JOURNAL OF CONTROLLED RELEASE, 2012, 161 (02) :693-702
[8]   In situ gel based on gellan gum as new carrier for nasal administration of mometasone furoate [J].
Cao, Shi-lei ;
Ren, Xiao-wei ;
Zhang, Qi-zhi ;
Chen, En ;
Xu, Feng ;
Chen, Jun ;
Liu, Li-Chun ;
Jiang, Xin-guo .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2009, 365 (1-2) :109-115
[9]   The effect of polymer coatings on physicochemical properties of spray-dried liposomes for nasal delivery of BSA [J].
Chen, K. H. ;
Di Sabatino, M. ;
Albertini, B. ;
Passerini, N. ;
Kett, V. L. .
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2013, 50 (3-4) :312-322
[10]   How much particle surface corrugation is sufficient to improve aerosol performance of powders? [J].
Chew, NYK ;
Tang, P ;
Chan, HK ;
Raper, JA .
PHARMACEUTICAL RESEARCH, 2005, 22 (01) :148-152
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