Abstract:
:Development of an oral docetaxel formulation has been hindered mainly due to its poor solubility and oral bioavailability. The aim of this study was to develop poloxamer F68/P85-based solid dispersions (SDs) for the oral delivery of docetaxel and investigate their in vivo pharmacokinetic impacts on the systemic absorption of docetaxel given orally, in comparison with a SD based on F68 alone. The F68 and/or P85-based docetaxel SDs were prepared with varying the contents of poloxamers and then evaluated in terms of morphology, crystallinity, solubility, dissolution, permeation across rat intestinal segments, and oral pharmacokinetics in rats. As a result, the SDs successfully changed the crystalline properties of docetaxel and enhanced the drug solubility and dissolution. The SD prepared with F68 alone significantly enhanced the dissolution but not intestinal permeation of docetaxel, leading to only limited enhancement of oral bioavailability (1.39-fold increase). Notably, however, the F68/P85-based SD significantly enhanced both the dissolution and intestinal permeation of docetaxel, achieving a markedly improved oral bioavailability (2.97-fold increase). Therefore, the present results suggest that the intestinal permeation factor should be taken into account when designing SD formulations for the oral delivery of BCS class IV drugs including docetaxel, and that P85 could serve as a potential formulation excipient for enhancing the intestinal permeation of docetaxel.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Song CK,Yoon IS,Kim DDdoi
10.1016/j.ijpharm.2016.05.002subject
Has Abstractpub_date
2016-06-30 00:00:00pages
102-8issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(16)30368-4journal_volume
507pub_type
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