Abstract：
:Low molecular weight heparins (LMWHs) have risen in popularity over the past decades. Owing to their appropriate pharmacokinetic profile, they enable long-term clinical applications, e.g. prophylaxis of deep vein thrombosis. Although the administration of LMWHs is not as frequent as of heparin, it still requires once daily injection at least. In order to prolong LMWH release, and thus provide less frequent subcutaneous administration, we designed and thoroughly evaluated thermoresponsive poloxamer-based systems combined with LMWH/chitosan pH-responsive nanocomplexes. A LMWH/chitosan mass ratio of 1:2 was the most appropriate for preparation of small, homogenous and stable nanocomplexes. Thermoresponsive hydrogels were examined by gelation temperature and time, thermal analysis, gel dissolution, LMWH release, and cytotoxicity in vitro. Hydrogels' behaviour was significantly shifted by gel composition e.g. the addition of hydroxypropylmethylcellulose to poloxamer-based systems decreased gelation temperature and time (from 28.6°C to 25.1°C and from 50s to 44s, respectively), but prolonged gel dissolution and LMWH release (7 and 4 days, respectively). Prolongation of drug release was additionally achieved with incorporation of LMWH/chitosan nanocomplexes into the gelling systems. As formulations demonstrated no cytotoxicity in vitro, it may be concluded that these double-responsive platforms are promising candidates for prolonged subcutaneous LMWH delivery during long-term treatment.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Radivojša Matanović M,Grabnar I,Gosenca M,Grabnar PAdoi
10.1016/j.ijpharm.2015.04.063subject
Has Abstractpub_date
2015-07-05 00:00:00pages
127-35issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(15)00371-3journal_volume
488pub_type
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