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    Amorphous Ropinirole-Loaded Mucoadhesive Buccal Film: A Potential Patient-Friendly Tool to Improve Drug Pharmacokinetic Profile and Effectiveness

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    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/cm 2·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

    Solid and Semisolid Innovative Formulations Containing Miconazole-Loaded Solid Lipid Microparticles to Promote Drug Entrapment into the Buccal Mucosa

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    The currently available antifungal therapy for oral candidiasis (OC) has various limita- tions restricting its clinical use, such as short retention time, suboptimal drug concentration and low patients compliance. These issues could be overcome using micro or nanotechnology. In par- ticular, solid lipid microparticles (SLMs) resulted as a particularly promising penetration enhancer carrier for lipophilic drugs, such as the antifungal miconazole (MCZ). Based on these considera- tions, cetyl decanoate (here synthesized without the use of metal catalysis) was employed together with 1-hexadecanol to prepare MCZ-loaded SLMs. These resulted in a powder composed of 45–300 μm diameter solid spherical particles, able to load a high amount of MCZ in the amorphous form and characterized by a melting temperature range perfectly compatible with oromucosal admin- istration (35–37 °C). Moreover, when compared to Daktarin ® 2% oral gel in ex vivo experiments, SLMs were able to increase up to three-fold MCZ accumulation into the porcine buccal mucosa. The prepared SLMs were then loaded into a buccal gel or a microcomposite mucoadhesive buccal film and evaluated in terms of MCZ permeation and/or accumulation into porcine buccal mucosa by using lower doses than the conventional dosage form. The promising results obtained high- lighted an enhancement in terms of MCZ accumulation even at low doses. Furthermore, the pre- pared buccal film was eligible as stable, reproducible and also highly mucoadhesive. Therefore, the formulated SLMs represent a penetration enhancer vehicle suitable to reduce the dose of lipophilic drugs to be administered to achieve the desired therapeutic effects, as well as being able to be ef- fectively embedded into easily administrable solid or semisolid dosage forms

    From the waste of must clarification to the production of a high polyphenols’ rich buccal film: new insight to treat oral oxidative stress-related pathologies

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    Introduction: To support drugs’ treatment of oral oxidative stress-related patologies polyphenols can be ideal candidates due to their antioxidant and antinflammatory activities1. A liquid polyphenols’ enriched excipient could be obtained by virtuous recovery of waste black bentonite (BB) coming from white grape must filtration2. Material & Methods: Both the BB-wet (starting waste as supplied) and BB-dry (after freeze-drying) were subjected to 7 consecutive cycles of green extraction by maceration with PEG200 as unconventional and innovative green solvent.The extracts were characterized by HPLC-DAD analysis, Folin-Ciocalteu, Bradford and DPPH assays. A thin buccal film was prepared by solvent casting using pectin as matrix polymer, calcium lactate and the best extract. Results: The multiple maceration procedure greatly enrich PEG200 in polyphenols. The best product was obtained from the BB-wet (third extraction step) and resulted in a solvent recovery >40% and GAE ≈ 4 mg/g. Consequently, it was directly used to prepare a soft, deformable and homogeneo buccal film. Conclusion: The valorization of the waste BB could be a virtuous approach to recover polyphenols. The consecutive multiple green maceration process produced a highly polyphenols’ rich secondary raw material directly useful to produce buccal films potentially promising to locally treat several oxidative stress-related oral pathologies
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