New prospective in treatment of Parkinson's disease: Studies on permeation of ropinirole through buccal mucosa

De, Viviana; Giandalia, Giulia; Siragusa, Maria Gabriella; Sutera, Flavia Maria; Giannola, Libero Italo

doi:10.1016/j.ijpharm.2012.03.022

Cited by 38 publications

(22 citation statements)

References 25 publications

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“…Mucosal specimens consisted of tissue removed from the ventral surface of the tongue of freshly slaughtered domestic pigs. Specimens were prepared as described previously [ 17 ]. Briefly, specimens, used within 2 h from animal sacrifice, were dipped for approximately 1 min in saline solution previously warmed to 60 °C; the connective tissue was then carefully peeled off from the mucosa (slides 150 ± 25 µm thick) to obtain the heat-separated epithelium along with the intact basal lamina.…”

Section: Methodsmentioning

confidence: 99%

“…Oral mucosal drug delivery is an alternative and promising method of systemic delivery which offers several advantages [ 17 , 18 ]. The oral mucosa is highly vascularized; for this reason, drugs that are absorbed through it directly enter the systemic circulation, bypassing the gastrointestinal tract and first-pass metabolism in the liver.…”

Section: Introductionmentioning

confidence: 99%

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Development and Characterization of an Amorphous Solid Dispersion of Furosemide in the Form of a Sublingual Bioadhesive Film to Enhance Bioavailability

Ajovalasit

Sutera³

et al. 2017

Pharmaceutics

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Administered by an oral route, Furosemide (FUR), a diuretic used in several edematous states and hypertension, presents bioavailability problems, reported as a consequence of an erratic gastrointestinal absorption due to various existing polymorphic forms and low and pH-dependent solubility. A mucoadhesive sublingual fast-dissolving FUR based film has been developed and evaluated in order to optimize the bioavailability of FUR by increasing solubility and guaranteeing a good dissolution reproducibility. The Differential Scanning Calorimetry (DSC) analyses confirmed that the film prepared using the solvent casting method entrapped FUR in the amorphous state. As a solid dispersion, FUR increases its solubility up to 28.36 mg/mL. Drug content, thickness, and weight uniformity of film were also evaluated. The measured Young’s Modulus, yield strength, and relative elongation of break percentage (EB%) allowed for the classification of the drug-loaded film as an elastomer. Mucoadhesive strength tests showed that the force to detach film from mucosa grew exponentially with increasing contact time up to 7667 N/m2. FUR was quickly discharged from the film following a trend well fitted with the Weibull kinetic model. When applied on sublingual mucosa, the new formulation produced a massive drug flux in the systemic compartment. Overall, the proposed sublingual film enhances drug solubility and absorption, allowing for the prediction of a rapid onset of action and reproducible bioavailability in its clinical application.

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Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Development and Characterization of an Amorphous Solid Dispersion of Furosemide in the Form of a Sublingual Bioadhesive Film to Enhance Bioavailability

Ajovalasit

Sutera³

et al. 2017

Pharmaceutics

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“…Simulated in vitro digestion, which mimics physicochemical and biochemical changes that occur in the upper gastrointestinal tract, was performed ( n = 6) as described by Tesoriere et al with the exception that a buffered pH 6.8 solution simulating saliva was prepared using NaCl (0.126 g), KCl (0.964 g), KSCN (0.189 g), KH 2 PO 4 (0.655 g), urea (0.200 g), Na 2 SO 4 ·10H 2 O (0.763 g), NH 4 Cl (0.178 g), CaCl 2 ·2H 2 O (0.228 g) and NaHCO 3 (0.631 g) in 1 L of distilled water …”

Section: Methodsmentioning

confidence: 99%

Quality, functional and sensory evaluation of pasta fortified with extracts from Opuntia ficus‐indica cladodes

et al. 2019

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BACKGROUND: The stems of Opuntia ficus-indica, known as cladodes, are a rich source of soluble fibers, which makes them an important candidate for the production of functional foods. Tagliatelle of durum wheat fortified with Opuntia cladode extract (OCE) at different levels of addition (10-30%, v/w) was prepared on a laboratory scale and quality characteristics and sensory acceptability were assessed. RESULTS:The main quality parameters (optimal cooking time, swelling index, cooking loss, dry matter) and sensory analysis on a nine-point hedonic scale were comparable with those of the control pasta sample (no added OCE) when durum wheat was supplemented with OCE at up to 20% (v/w). An in vitro human simulated gastrointestinal digestion in the presence of cholesterol or its main dietary oxidized derivative, 7-ketocholesterol, showed that OCE-fortified pasta strongly reduced the bioaccessibility of both the sterols (the higher the incorporated OCE level, the higher the effect). Moreover the extent of starch digestion decreased with increasing levels of OCE. CONCLUSION:The results of the present study indicate that OCE-fortified pasta comprises a food with healthy properties, such as blood cholesterol-and glucose-lowering capabilities.

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“…Excesses of connective and adipose tissue were trimmed away. Specimens were dipped for approximately 1 min in a pre-warmed (60°C) saline solution; the connective tissue was then carefully peeled off from the mucosa (slides 250 ± 25 mm thick) to obtain the heat-separated epithelium along with the intact basal lamina (35). The thickness was measured using a digital micrometer.…”

Section: Ex Vivo Permeation/penetration Studies Of Barbaloin From Matmentioning

confidence: 99%

Mucoadhesive Polymeric Films to Enhance Barbaloin Penetration Into Buccal Mucosa: a Novel Approach to Chemoprevention

Prima

Conigliaro

2019

AAPS PharmSciTech

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Nowadays, chemoprevention by administering natural supplements is considered an attractive strategy to reverse, suppress, or prevent the evolution of premalignant oral lesions. In particular, Barbaloin exhibits anti-proliferative, anti-inflammatory, and anti-cancer properties, and it results useful in multi-therapy with classic chemotherapeutics. Therefore, in this work, mucoadhesive buccal films, as locoregional drug delivery system able to provide a targeted and efficient therapeutic delivery of Barbaloin, are proposed. Thus, Aloin extractloaded Eudragit® RL100 or Eudragit® RS100-based buccal films were designed in order to obtain an easily self-administrable formulation capable of promoting Barbaloin penetration into buccal mucosa and assuring high patient compliance. Large amounts of extract (44%) were loaded into the polymer matrix and six formulations were prepared varying polymers and plasticizers ratios. For all formulations, physical form (thermogravimetric analysisdifferential scanning calorimetry, TGA-DSC), swelling degree, mucoadhesiveness, drug release, and ability to promote drug penetration in mucosa have been investigated. After a sequential selection process, Eudragit RS 100-based film, with low PVP and high plasticizers amounts, emerged as the most promising. It results appropriately flexible, uniform in terms of weight, thickness and drug content, as well as characterized by suitable surface pH, good mucoadhesiveness, and low swelling degree. It displays a Higuchian drug release behavior up to 89% of Barbaloin released, thus demonstrating that diffusion through the matrix is the main release mechanism. Remarkable penetration enhancer properties of film were demonstrated by evidence of Barbaloin accumulation into buccal mucosa up to 10-fold higher than those obtained following administration of Aloin solution.

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New prospective in treatment of Parkinson's disease: Studies on permeation of ropinirole through buccal mucosa

Cited by 38 publications

References 25 publications

Development and Characterization of an Amorphous Solid Dispersion of Furosemide in the Form of a Sublingual Bioadhesive Film to Enhance Bioavailability

Development and Characterization of an Amorphous Solid Dispersion of Furosemide in the Form of a Sublingual Bioadhesive Film to Enhance Bioavailability

Quality, functional and sensory evaluation of pasta fortified with extracts from Opuntia ficus‐indica cladodes

Mucoadhesive Polymeric Films to Enhance Barbaloin Penetration Into Buccal Mucosa: a Novel Approach to Chemoprevention

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