Inulin based micelles loaded with curcumin or celecoxib with effective anti-angiogenic activity

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• 作者：Delia Mandracchia^a ; ¹ ; Giuseppe Tripodo^b ; ¹ ; ^{giuseppe.tripodo@unipv.it" class="auth_mail" title="E-mail the corresponding author} ; Adriana Trapani^a ; Simona Ruggieri^c ; Tiziana Annese^c ; Theodora Chlapanidas^b ; Giuseppe Trapani^a ; Domenico Ribatti^c ; ^d
• 关键词：Inulin (PubChem CID ; 16219508) ; Vitamin E (PubChem CID ; 14985) ; Vitamin E Succinate (PubChem CID ; 20353) ; Celecoxib (PubChem CID ; 2662) ; Curcumin (PubChem CID ; 969516)
• 刊名：European Journal of Pharmaceutical Sciences
• 出版年：2016
• 出版时间：10 October 2016
• 年：2016
• 卷：93
• 期：Complete
• 页码：141-146
• 全文大小：628 K

文摘

Curcumin (CUR) and celecoxib (CLX) are two highly hydrophobic drugs which show bioavailability problems due to their poor aqueous solubility. The aim of this study was to encapsulate each of these drugs in micelles based on biodegradable and amphiphilic polymers to investigate their anti-angiogenesis activity. Here we use an amphiphilic polymer, based on two natural substances from renewable resources (Inulin and Vitamin E, INVITE), as a self-assembling system for the drug delivery of CUR and CLX. By the in vivo assay of chick embryo chorioallantoic membrane (CAM) it was assessed that both INVITE-CUR and INVITE-CLX micelles possess remarkable anti-angiogenic activity, while the INVITE micelles alone resulted intrinsically pro-angiogenic. Furthermore, it has been shown that encapsulation of CUR and CLX in INVITE micelles enhances of several magnitudes the water-solubility of CUR and CLX (14·10⁵ and 3·10² times for CUR and CLX, respectively).

These results may have interesting implications not only in anticancer or diabetic maculopathy therapy based on the anti-angiogenesis strategy but also for regenerative medicine where over-production of new vessels is required.