Hillaireau H, Le Doan T, Chacun H, Janin J, Couvreur P
Universite Paris Sud, UMR CNRS 8612, 5 rue J.B. Clément, 92296 Châtenay-Malabry, France.
Int J Pharm. 2007 Mar 1;331(2):148-52. doi: 10.1016/j.ijpharm.2006.10.031. Epub 2006 Oct 27.
In a previous study, we have shown that cidofovir (CDV) and azidothymidine-triphosphate (AZT-TP) were poorly encapsulated in poly(iso-butylcyanoacrylate) (PIBCA) aqueous-core nanocapsules. This was attributed to the rapid leakage of these small and hydrophilic molecules through the thin polymer wall of the nanocapsules. In the present study, we have selected various water-soluble polymers as increasing Mw adjuvants and investigated their influence on the entrapment of mononucleotides (CDV, AZT-TP) as well as of oligonucleotides (ODN) into these PIBCA aqueous-core nanocapsules. We show here that the presence of cationic polymers (i.e. poly(ethyleneimine) (PEI) or chitosan) in the nanocapsule aqueous compartment allowed successful encapsulation of AZT-TP and ODN.
在先前的一项研究中,我们已经表明,西多福韦(CDV)和叠氮胸苷三磷酸(AZT-TP)在聚异丁基氰基丙烯酸酯(PIBCA)水核纳米胶囊中的包封率很低。这归因于这些小分子和亲水分子通过纳米胶囊的薄聚合物壁快速泄漏。在本研究中,我们选择了各种水溶性聚合物作为分子量增加助剂,并研究了它们对单核苷酸(CDV、AZT-TP)以及寡核苷酸(ODN)包封到这些PIBCA水核纳米胶囊中的影响。我们在此表明,纳米胶囊水相隔室中阳离子聚合物(即聚乙烯亚胺(PEI)或壳聚糖)的存在使得AZT-TP和ODN能够成功包封。