Electrospun fibers as potential carrier systems for enhanced drug release of perphenazine

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• 作者：Giovanna Bruni^a ; ^{giovanna.bruni@unipv.it" class="auth_mail" title="E-mail the corresponding author} ; Lauretta Maggi^b ; Loredana Tammaro^c ; ¹ ; Rosadele Di Lorenzo^a ; Valeria Friuli^b ; Sharon D⿿Aniello^c ; Mariarosa Maietta^a ; Vittorio Berbenni^a ; Chiara Milanese^a ; Alessandro Girella^a ; Amedeo Marini^a
• 关键词：Electrospinning ; Perphenazine ; Solubility ; Dissolution rate ; Polymeric drug carrier ; Amorphous
• 刊名：International Journal of Pharmaceutics
• 出版年：2016
• 出版时间：10 September 2016
• 年：2016
• 卷：511
• 期：1
• 页码：190-197
• 全文大小：2309 K

文摘

Solubility represents an important challenge for formulation of drugs, because the therapeutic efficacy of a drug depends on the bioavailability and ultimately on its solubility. Low aqueous solubility is one of the main issues related with formulation design and development of new molecules. Many drug molecules present bioavailability problems due to their poor solubility. For this reason there is a great interest in the development of new carrier systems able to enhance the dissolution of poorly water-soluble drugs.

In this work, fibers containing an insoluble model drug and prepared by an electrospinning method, are proposed and evaluated to solve this problem. Two hydrophilic polymers, polyvinylpyrrolidone (Plasdone® K29/32) and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus®) were used to increase the water solubility of perphenazine.

The physico-chemical characterization suggests that the drug loaded in the fibers is in the amorphous state. Both polymeric carriers are effective to promote the drug dissolution rate in water, where this active pharmaceutical ingredient is insoluble, due to the fine dispersion of the drug into the polymeric matrices, obtained with this production technique. In fact, the dissolution profiles of the fibers, compared to the simple physical mixture of the two components, and to the reference commercial product Trilafon® 8 mg tablets, show that a strong enhancement of the drug dissolution rate can be achieved with the electrospinning technique.