Novel pH-sensitive interpenetrated network polyspheres of polyacrylamide-g-locust bean gum and sodium alginate for intestinal targeting of ketoprofen: In vitro and in vivo evaluation

被引:22
作者
Boppana, Rashmi [1 ]
Raut, Sushil Yadaorao [2 ]
Mohan, G. Krishna [3 ]
Sa, Biswanath [4 ]
Mutalik, Srinivas [2 ]
Reddy, Kakarla Raghava [5 ]
Das, Kusal K. [6 ]
Biradar, Mallanagouda S. [7 ]
Kulkarni, Raghavendra V. [1 ]
机构
[1] BLDE Univ Campus, BLDEAs SSM Coll Pharm & Res Ctr, Dept Pharmaceut & Pharmaceut Technol, Vijayapur 586103, India
[2] Manipal Acad Higher Educ, Manipal Coll Pharmaceut Sci, Dept Pharmaceut, Manipal 576104, Karnataka, India
[3] Jawaharlal Nehru Technol Univ, Ctr Pharmaceut Sci, Hyderabad 500585, India
[4] Jadavpur Univ, Dept Pharmaceut Technol, Kolkata 700032, India
[5] Univ Sydney, Sch Chem & Biomol Engn, Sydney, NSW 2006, Australia
[6] BLDE Deemed Univ, Shri BM Patil Med Coll Hosp & Res Ctr, Dept Physiol, Vijayapur 586103, India
[7] BLDE Deemed Univ, Shri BM Patil Med Coll Hosp & Res Ctr, Dept Med, Vijayapur 586103, India
关键词
Intestinal drug targeting; Graft copolymer; Interpenetrated network polyspheres; In-vivo studies; Ketoprofen; MICROWAVE-ASSISTED SYNTHESIS; CONTROLLED-RELEASE; HYDROGEL BEADS; ANTIMICROBIAL ACTIVITY; MICROSPHERES; DELIVERY; ACRYLONITRILE; CHITOSAN; ALCOHOL);
D O I
10.1016/j.colsurfb.2019.04.060
中图分类号
Q6 [生物物理学];
学科分类号
071011 ;
摘要
In this report, novel pH-sensitive interpenetrated network (IPN) polyspheres were developed utilizing polyacrylamide-g-locust bean gum (PAAm-g-LBG) in combination with sodium alginate (SA) to achieve intestinal targeted delivery of ketoprofen. PAAm-g-LBG was synthesized under microwave irradiation wherein ceric ammonium nitrate was used as reaction initiator and then conversion of PAAm-g-LBG as pH-sensitive copolymer was carried out by alkaline hydrolysis. The PAAm-g-LBG copolymer was characterized through H-1-NMR, FTIR and elemental analysis. The IPN polyspheres exhibited pH-depended swelling or de-swelling with the alteration of surrounding pH. The in-vitro release of drug from IPN polyspheres was found to be higher (approximate to 90%) in phosphate buffer of pH 7.4 in comparison with that in pH 1.2 buffer (10.6%). The in-vivo pharmacokinetic, anti-inflammatory screening and stomach histopathology studies performed on Wistar rats revealed pH sensitivity of IPN polyspheres where ketoprofen was successfully targeted to small intestine resulting in reduced side effects of ketoprofen like ulcer formation, erosion of gastric mucosa and hemorrhages.
引用
收藏
页码:362 / 370
页数:9
相关论文
共 36 条
[1]   In vivo evaluation of zidovudine (AZT)-loaded ethylcellulose microspheres after oral administration in Beagle dogs [J].
AbuIzza, K ;
Tambrallo, L ;
Lu, DR .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1997, 86 (05) :554-559
[2]   Development of novel interpenetrating network gellan gum-poly(vinyl alcohol) hydrogel microspheres for the controlled release of carvedilol [J].
Agnihotri, SA ;
Aminabhavi, TM .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 2005, 31 (06) :491-503
[3]   Controlled release of cephalexin through gellan gum beads: Effect of formulation parameters on entrapment efficiency, size, and drug release [J].
Agnihotri, Sunil A. ;
Jawalkar, Sheetal S. ;
Aminabhavi, Tejraj M. .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2006, 63 (03) :249-261
[4]   Pilot study of relative bioavailability of two oral formulations of ketoprofen 25 mg in healthy subjects. A fast-dissolving lyophilized tablet as compared to immediate release tablet [J].
Ahmed, I. S. ;
Fatahalla, F. A. .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 2007, 33 (05) :505-511
[5]   Functionally modified polyacrylamide-graft-gum karaya pH-sensitive spray dried microspheres for colon targeting of an anti-cancer drug [J].
Alange, Vijaykumar V. ;
Birajdar, Ravindra P. ;
Kulkarni, Raghavendra V. .
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES, 2017, 102 :829-839
[6]   In vitro and in vivo studies of ibuprofen-loaded biodegradable alginate beads [J].
Arica, B ;
Çalis, S ;
Atilla, P ;
Durlu, NT ;
Çakar, N ;
Kas, HS ;
Hincal, AA .
JOURNAL OF MICROENCAPSULATION, 2005, 22 (02) :153-165
[7]   Interpenetrating network hydrogel beads of carboxymethylcellulose and egg albumin for controlled release of lipid lowering drug [J].
Boppana, Rashmi ;
Kulkarni, Raghavendra V. ;
Mutalik, Srinivas S. ;
Setty, C. Mallikarjun ;
Sa, Biswanath .
JOURNAL OF MICROENCAPSULATION, 2010, 27 (04) :337-344
[8]   Sustained release of human growth hormone from PLGA solution depots [J].
Brodbeck, KJ ;
Pushpala, S ;
McHugh, AJ .
PHARMACEUTICAL RESEARCH, 1999, 16 (12) :1825-1829
[9]   Poly(vinyl alcohol)-graft-polyacrylamide with different grafts number and length as studied by 1H NMR spectroscopy [J].
Demehenko, O ;
Zheltonozhskaya, T ;
Turov, A ;
Tsapko, M ;
Syromyatnikov, V .
MOLECULAR CRYSTALS AND LIQUID CRYSTALS, 2005, 427 (427) :537-545
[10]  
Donawade DS, 2006, INDIAN J CHEM B, V45, P689