Amorphous Ropinirole-Loaded Mucoadhesive Buccal Film: A Potential Patient-Friendly Tool to Improve Drug Pharmacokinetic Profile and Effectiveness.
Amorphous Ropinirole-Loaded Mucoadhesive Buccal Film: A Potential Patient-Friendly Tool to Improve Drug Pharmacokinetic Profile and Effectiveness.
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DOI：
10.3390/jpm10040242
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发表时间：
2020-11-25
影响因子：
--
通讯作者：
De Caro V
中科院分区：
文献类型：
--
作者：
Di Prima G;Campisi G;De Caro V
目前，治疗帕金森病的策略仅仅是症状性的，包括给予左旋多巴和/或多巴胺受体激动剂。其中，罗匹尼罗（ropininirole， ROP）是一种广泛口服给药的分子，尽管它对肝脏代谢非常敏感。由于文献报道口腔黏膜是ROP给药的潜在有效途径，因此开发新颖、有效、舒适的口腔黏膜制剂应被证明是可取的，以提高药物的治疗效果，并允许能够满足患者需求的个性化治疗策略。结果表明，该新型ROP膜具有一定的柔韧性；统一的;表面pH适宜；好mucoadhesiveness;溶胀度低；并且快速，完全释放药物。此外，在面积为0.282 cm2、剂量为2.29 mg的膜上进行离体评估后，经口腔黏膜的药物通量与根据文献计算的ROP- pr口服4mg后稳态状态下到达血流的ROP量非常接近（分别为0.237 mg/cm2·h−1和0.243 mg/h）。此外，药物通量和ROP剂量可以根据患者的需要，通过改变给药的磁盘面积来精确地随时间调节。此外，所提出的ROP膜没有延迟时间，在血液中立即产生药物输入，这可能导致迅速的治疗反应。这些发现使ROP膜成为一种潜在的舒适和患者友好的配方，并且是进一步临床试验的有希望的候选者。
Nowadays the therapeutic strategies to manage Parkinson’s Disease are merely symptomatic and consist of administering L-DOPA and/or dopamine receptor agonists. Among these, Ropinirole (ROP) is a widely orally-administered molecule, although it is extensively susceptible to hepatic metabolism. Since literature reports the buccal mucosa as a potentially useful route to ROP administration, the development of novel, effective, and comfortable oromucosal formulations should prove desirable in order to both enhance the therapeutic efficacy of the drug and allow a personalized therapeutic strategy able to meet the patient’s needs. The results of the proposed ROP film as a new dosage form show that it is flexible; uniform; and characterized by suitable surface pH; good mucoadhesiveness; low swelling degree; and fast, complete drug release. Moreover, after ex vivo evaluation on a film having an area of 0.282 cm2 and dose of 2.29 mg, the results of drug flux through the buccal mucosa are closely comparable to the amount of ROP that reaches the bloodstream at the steady-state condition after ROP-PR 4 mg oral administration, calculated according to the literature (0.237 mg/cm2·h−1 vs. 0.243 mg/h, respectively). Moreover, drug flux and ROP dose could be accurately modulated time-by-time depending on the patient’s need, by varying the administered disk area. In addition, the proposed ROP film displays no lag time, producing an immediate drug input in the bloodstream, which could result in a prompt therapeutic response. These findings make ROP film a potentially comfortable and patient-friendly formulation, and a promising candidate for further clinical trials.
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影响因子：
4.7
作者：
Murgia D;Angellotti G;Conigliaro A;Carfi Pavia F;D'Agostino F;Contardi M;Mauceri R;Alessandro R;Campisi G;De Caro V
通讯作者：
De Caro V
影响因子：
5.4
作者：
De Caro, Viviana;Murgia, Denise;Campisi, Giuseppina
通讯作者：
Campisi, Giuseppina
影响因子：
168.9
作者：
Kalia, Lorraine V.;Lang, Anthony E.
通讯作者：
Lang, Anthony E.
影响因子：
8.6
作者：
Grosset, KA;Bone, I;Grosset, DG
通讯作者：
Grosset, DG
DOI：
10.1016/j.pnpbp.2020.109942
发表时间：
2020-08-30
影响因子：
5.6
作者：
Napier, T. Celeste;Kirby, Alana;Persons, Amanda L.
通讯作者：
Persons, Amanda L.