Bhowmik Manas, Kumari Puja, Sarkar Gunjan, Bain Mrinal Kanti, Bhowmick Biplab, Mollick Md Masud Rahaman, Mondal Dibyendu, Maity Dipanwita, Rana Dipak, Bhattacharjee Debashis, Chattopadhyay Dipankar
Himalayan Pharmacy Institute, Sikkim University, Majhitar, Rangpo, East Sikkim 737136, India.
Int J Biol Macromol. 2013 Nov;62:117-23. doi: 10.1016/j.ijbiomac.2013.08.024. Epub 2013 Aug 26.
The aim of this investigation was to develop a novel in situ gelling formulation based on poloxamer-407 (PM) for the sustained release of an ophthalmic drug. In an attempt to reduce the concentration of PM without compromising the in situ gelling capability and also to increase the drug release time, xanthan gum (XG) and guar gum (GG) were added into PM to develop different formulations. At concentrations of 18% and above, the PM was able to undergo sol-gel transition below body temperature. It was found that XG and GG at a weight ratio of 3:7 were able to convert PM solution into gel below body temperature at PM concentrations below 18%. Both the in vitro and in vivo studies indicated that the PM with an XG-GG combination had a better ability to retain the drug than PM itself. The results indicated that the developed in situ gelling formulations containing PM with XG-GG may be a better alternative than a conventional eye drop.
本研究的目的是开发一种基于泊洛沙姆-407（PM）的新型原位凝胶制剂，用于眼科药物的缓释。为了在不影响原位凝胶化能力的情况下降低PM的浓度，并延长药物释放时间，将黄原胶（XG）和瓜尔胶（GG）添加到PM中以开发不同的制剂。在18%及以上的浓度下，PM能够在体温以下发生溶胶-凝胶转变。研究发现，在PM浓度低于18%时，重量比为3:7的XG和GG能够在体温以下将PM溶液转化为凝胶。体外和体内研究均表明，含有XG-GG组合的PM比PM本身具有更好的药物保留能力。结果表明，所开发的含有PM与XG-GG的原位凝胶制剂可能是比传统滴眼液更好的替代品。
