In this study solid dispersions of carbamazepine in the hydrophilic Kollidon® VA64 polymer, adsorbed onto Neusilin® UFL2 adsorption carrier have been employed to improve carbamazepine dissolution rate. In order to evaluate effects of changing in the proportions of all solid dispersion components on carbamazepine dissolution rate, D-optimal mixture experimental design was used in the formulation development. From all prepared solid dispersion formulations, significantly faster carbamazepine dissolution was observed compared to pure drug. Ternary solid dispersions containing carbamazepine, Kollidon® VA64 and Neusilin® UFL2 showed superior dissolution performances over binary ones, containing only carbamazepine and Neusilin® UFL2. Proportion of Kollidon® VA64 showed the most profound effect on the amount of carbamazepine dissolved after 10 and 30 min, whereby these parameters increase upon increasing in Kollidon® VA64 concentrations up to the middle values in the studied range of Kollidon® VA64 concentrations. Physicochemical characterization of the selected samples using differential scanning calorimetry, FT-IR spectroscopy, powder X-ray diffraction and polarizing light microscopy showed polymorphic transition of carbamazepine from more thermodynamically stable monoclinic form (form III) to less thermodynamically stable triclinic form (form I) in the case of ternary, but not of binary solid dispersion formulations. This polymorphic transition can be one of the factors responsible for improving of carbamazepine dissolution rate from studied solid dispersions. Ternary solid dispersions prepared with Kollidon® VA64 hydrophilic polymer and Neusilin® UFL2 adsorption carrier resulted in significantly improvement of carbamazepine dissolution rate, but formation of metastable polymorphic form of carbamazepine requires particular care to be taken in ensuring product long term stability.
Acne vulgaris (acne) is chronic inflammatory dermatosis which affects the pilosebaceous unit, with a varied clinical picture including inflammatory and non-inflammatory cutaneous lessions. This multifactorial disease mostly occurs in adolescents; however, it can also affect children and adults. Different therapy options for acne treatment exist, comprising topical, systemic and hormonal agents or a combination thereof. The choice of the therapy depends on various factors, for instance the severity and extent of the disease and site of involvement. Commonly used topical acne therapies include benzoyl peroxide, salicylic acid, antibiotics, retinoids, azelaic acid, sulfone agents and their combinations. Systemic antibiotics are indicated for use in moderate to severe inflammatory acne and should be used in combination with a topical retinoid and benzoyl peroxide. The available conventional formulations often cause side effects such as skin irritation, dryness, peeling, itching, leading to reduced patient compliance and compromised therapeutical efficacy. Novel drug delivery systems are promising option for improved acne treatment outcome, as they can diminish the side effects caused by the therapeutic agents or can modulate their properties and at the same time offering possibilities for modified release and improved skin penetration of the active substances. The cosmetics manufacturers implement micro/nanotechnology in their formulations, while patent protection for cosmetics has gained more importance over the past decades. This review focuses on micro/nanoparticulated carrier systems that can be used for acne treatment and the published patents concerning them.
Carbamazepine belongs to the class II biopharmaceutical classification system (BCS) which is characterized by a high per-oral dose, a low aqueous solubility and a high membrane permeability. The bioavailability of such a drug is limited by the dissolution rate. The present study deals with the formulations of immediate release tablets of poorly soluble carbamazepine. As model tablets for this investigation, two formulations (named "A" and "B" formulations) of carbamazepine tablets labeled to contain 200 mg were evaluated. The aim of this study was to establish possible differences in dissolution profile of these two formulations purchased from the local market. The increased crystallinity together with enlarged particle size, enhanced aggregation and decreased wettability of the drug, resulted in insufficient dissolution rate for formulation "B". From the dissolution point of view, this formulation was inferior to the formulation "A", due to the solubilization effect.
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