Release of Ropinirole in Acrylate Transdermal Patches: Mutual Interactions Between Formulation Variables.

The aim of this study is to evaluate the cooperative interactions between formulation variables of ropinirole transdermal patches and characterize the effects of drug loading and crystallinity, degree of ionization and drug-polymer solubilization, functionalization of acrylate polymeric basis, and the addition of permeation enhancers over the release profiles. Several series of transdermal films based on carboxylic or hydroxylic acrylates (DuroTak®) and containing 1 to 10% ropinirole hydrochloride were laminated by mold-casting and evaporation. Formulations were characterized for crystallinity, drug particle size, drug assay, and residual solvents.

Biopharmaceutic study and efficacy of natural and derivatives flavanones formulations.

The development and characterization of nanostructured flavanone formulations (FF) of extracted from and , , and derivatives by structural modification of as anti-inflammatory candidates for topical treatment of local inflammation. The FF were physicochemical characterized and the behavior release, permeation and, anti-inflammatory efficacy in the rat model were studied. The FF revealed sustained drug release and showed slow drug penetration in human skin.

Carprofen Permeation Test through Porcine Ex Vivo Mucous Membranes and Ophthalmic Tissues for Tolerability Assessments: Validation and Histological Study.

Carprofen (CP), a non-steroidal anti-inflammatory drug (NSAID), is profusely used in veterinary medicine for its analgesic and anti-inflammatory activity. Some undesirable effects are associated with its systemic administration. Alternative local routes are especially useful to facilitate its administration in animals.

Ex Vivo Permeation of Carprofen Vehiculated by PLGA Nanoparticles through Porcine Mucous Membranes and Ophthalmic Tissues.

(1) Background: Carprofen (CP), 2-(6-chlorocarbazole) propionic acid, is used as an anti-inflammatory, analgesic and anti-pyretic agent and it belongs to the family of non-steroidal anti-inflammatory drugs (NSAIDs). CP has some adverse reactions in systemic administration; for this reason, topical administration with CP nanoparticles (CP-NPs) can be an optimal alternative. The main objective of this work is the investigation of ex vivo permeation of CP through different types of porcine mucous membranes (buccal, sublingual and vaginal) and ophthalmic tissues (cornea, sclera and conjunctiva) to compare the influence of CP-NPs formulation over a CP solution (CP-Solution).

Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery.

Efficient topical delivery of imidazolic antifungals faces the challenge of overcoming its limited water solubility and its required long-lasting duration of treatments. In this paper, a hydrophilic multiple emulsion (ME) of Bifonazole (BFZ) is shown to maximize its skin retention, minimize its skin permeation, and maintain an acceptable level of being harmless in vivo. The formulations were pharmaceutically characterized and application properties were assessed based on viscosity measurements.

Clotrimazole multiple W/O/W emulsion as anticandidal agent: Characterization and evaluation on skin and mucosae.

Clotrimazole (CLT) was formulated in a multiple W/O/W emulsion (ME) with the aim of evaluating its potential as topical anticandidal agent and comparing with marketed products. A previously evaluated CLT-ME was selected and physicochemically characterized. The in vitro release behavior and the ex vivo permeation profiles were assessed using Franz diffusion cells using three different types of biological membranes: human skin and porcine buccal, sublingual and vaginal mucosae.

Skin permeation of econazole nitrate formulated in an enhanced hydrophilic multiple emulsion.

Local delivery of imidazolic antifungals is limited by its extreme lipophilicity. Multiple emulsions (ME) are a potential vehicle to enhance the delivery of econazole nitrate (ECN), an antifungal targeted to deep-seated epidermal yeast infections. An 1% ECN hydrophilic ME was compared with a commercial formulation in terms of rheology, droplet size and in vitro antifungal activity against Candida species.

About the equivalence between different batches of a glycopeptide drug.

Context: Teicoplanin is a glycopeptide antibiotic consisting of a combination of different active components. Clinical equivalence between different batches of this drug is not guaranteed by the present pharmacopeial specification of chemical composition based on an HPLC chromatogram.

Objective: To test a modification of this specification and to evaluate independent compositions recently published in the literature.

Composition specification of teicoplanin based on its estimated relative bioavailability.

Context: Teicoplanin is a fermentative antibiotic consisting of several active components that contribute similarly to the antibacterial activity, but exhibit different pharmacokinetic properties. Differences in systemic exposure between batches of teicoplanin are possible within pharmacopeial specifications as the proportion of subcomponents may vary from batch to batch.

Objective: The aim of this paper is to study the possible modification of the present pharmacopeial specification for teicoplanin composition to ensure an a priori pharmacokinetic equivalence between all pharmacopoeial-compliant batches.

Relevance of equivalence assessment of topical products based on the dermatopharmacokinetics approach.

Common procedures to test bioequivalence of oral products, measuring the rate and extent of the obtained plasma levels, do not apply to drug products for topical use, which provide limited systemic absorption. Nowadays, clinical trials are still the goldenrule for the development of a generic topical product but, unfortunately, not many techniques are helpful for the specific investigation of in vivo topical absorption. Additionally, during early stages of pharmaceutical development, experimental procedures for demonstrating the quality by design of topical formulations are lacking.