Oxidative damage and inflammation have been pointed out in preclinical studies as the root cause of cancer and other chronic diseases such as diabetes, hypertension, Alzheimer’s disease, etc. Epidemiological and clinical studies have suggested that cancer could be prevented or significantly reduced by treatment with anti-oxidant and anti-inflammatory drugs, therefore, curcumin, a principal component of turmeric (a curry spice) showing strong anti-oxidant and anti-inflammatory activities, might be a potential candidate for the prevention and/or treatment of cancer and other chronic diseases. However, curcumin, a highly pleiotropic molecule with an excellent safety profile targeting multiple diseases with strong evidence on the molecular level, could not achieve its optimum therapeutic outcome in past clinical trials, largely due to its low solubility and poor bioavailability. Curcumin can be developed as a therapeutic drug through improvement in formulation properties or delivery systems, enabling its enhanced absorption and cellular uptake. This review mainly focuses on the anti-inflammatory potential of curcumin and recent developments in dosage form and nanoparticulate delivery systems with the possibilities of therapeutic application of curcumin for the prevention and/or treatment of cancer.

Abstract(Trans)dermal drug therapy is gaining increasing importance in the modern drug development. To fully utilize the potential of this route, it is important to optimize the delivery of active ingredient/drug into/through the skin. The optimal carrier/vehicle can enhance the desired outcome of the therapy therefore the optimization of skin formulations is often included in the early stages of the product development. A rational approach in designing and optimizing skin formulations requires well-defined skin models, able to identify and evaluate the intrinsic properties of the formulation. Most of the current optimization relies on the use of suitable ex vivo animal/human models.However, increasing restrictions in use and handling of animals and human skin stimulated the search for suitable artificial skin models. This review attempts to provide an unbiased overview of the most commonly used models, with emphasis on their limitations and advantages. The choice of the most applicable in vitro model for the particular purpose should be based on the interplay between the availability, easiness of the use, cost and the respective limitations.

The texture properties of formulation are an important parameter in optimization of topical formulations. These properties will affect applicability of the formulation at the administration site and therapy outcome. Our aim was to develop a fast and reliable method to characterize texture properties of hydrogels, namely cohesiveness, adhesiveness, and hardness. During the method development, we realized that the measurements setup needed to be adjusted for each hydrogel type, namely Carbopol, chitosan, and poloxamer hydrogels. The influence of the polymer concentration, pH, and incorporation of additives such as glycerol, drug solution, or liposomes on the texture properties, as determined by Texture Analyzer, was evaluated. In addition, the new method was applied to determine the changes during the accelerated stability testing. While Carbopol and poloxamer gels showed a linear relationship between the polymer concentration and texture properties, for low molecular weight chitosan gels the properties increased in exponential manner with increasing polymer concentration. The effect of incorporated liposomes on the gel properties was found to be dependent on the type of hydrogel. The hydrogel hardness was affected by the temperature as seen in accelerated stability testing. The method represents a valuable tool in pharmaceutical and cosmetics formulation development. © 2011 Wiley Periodicals, Inc. J Appl Polym Sci, 2012

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Resveratrol (RES), chemically known as 3,5,4'-trihydroxy-transstilbene, is a promising multi-targeted anti-oxidative and antiinflammatory natural polyphenol. Preclinical studies showed its biological activities against the pathogens of sexually transmitted diseases causing vaginal inflammation and infections. Due to its low solubility and poor bioavailability, the optimal therapeutic uses are limited. Therefore, a clinically acceptable topical vaginal formulation of RES exhibiting optimal therapeutic effects is highly desirable. For this purpose, we prepared and optimized chitosan-coated liposomes with RES. The coated vesicles (mean diameter 200 nm) entrapped up to 77% of RES, a sufficient load to assure required therapeutic outcome. In vitro drug release study showed the ability of liposomes to provide sustained release of RES. In vitro anti-oxidative activities of RES, namely DPPH and ABTS*+ radicals scavenging assays, confirmed RES to be as potent as standard anti-oxidants, vitamins C and E. The anti-oxidative activities of RES and its corresponding liposomal formulation were also compared by measuring enhanced superoxide dismutase (SOD) activities in lipopolysaccharide (LPS)-induced J774A.1 cells. In vitro antiinflammatory activities were compared by measuring nitric oxide (NO), tumor necrosis factor (TNF)-α and interleukin (IL)-1β production in LPSinduced J774A.1 cells. Liposomal RES was found to exhibit stronger antioxidative and anti-inflammatory activities than RES solution. Resveratrol (RES), chemically known as 3,5,4'-trihydroxy-trans-stilbene, is a 18 promising multi-targeted anti-oxidative and anti-inflammatory natural polyphenol. Preclinical 19 studies showed its biological activities against the pathogens of sexually transmitted diseases 20 causing vaginal inflammation and infections. Due to its low solubility and poor 21 bioavailability, the optimal therapeutic uses are limited. Therefore, a clinically acceptable 22 topical vaginal formulation of RES exhibiting optimal therapeutic effects is highly desirable. 7Corrections were made accordingly as mentioned on page 8, lines 210-217. 8 9Please discuss the possibility for using other polymers instead of chitosan. 11Some discussion was added on page 18, lines 551-555 12 13Spelling error -page 7, section 2.7., should be "Characterization…" instead of

16The choice of drug therapy in pregnant patients suffering from vaginal infections is limited 17 by the safety profile of the drug. Assuring the efficient topical therapy to avoid systemic 18 absorption is considered the best therapy option. Chitosan-coated liposomes have been 19 developed and optimized to assure localized therapy of clotrimazole. Chitosan was selected 20 as mucoadhesive polymer both to prolong system's retention at the vaginal site and act on 21 biofilms responsible for high recurrence of infections. Sonicated liposomes were coated 22 with chitosan in three different concentrations, namely 0.1, 0.3 and 0.6 % (w/v).

The aim of this work was to clarify the dynamics behind the influence of ionic strength on the changes in drug release from large unilamellar vesicles (LUVs). For this purpose, we have investigated the transport of two different model drugs (caffeine and hydrocortisone) formulated into liposomes through different types of barriers with different retention properties (regenerated cellulose and the newly introduced biomimetic barrier, Permeapad ®). Drug release from liposomes was studied utilizing the standard Franz diffusion cells. LUV dispersions were exposed to the isotonic, hypotonic and hypertonic environment (difference of 300 mOsm/kg between the initial LUVs and the environment) and experimental data treated with both linear and nonlinear (Korsmeyer-Peppas) regression models. To alter the rigidity of the liposomal membranes, cholesterol was introduced in the liposomal barriers (up to 25% w/w). Korsmeyer-Peppas model was proven to be suited to analyse experimental data throughout the experimental time frame, providing important additive information in comparison to standard linear approximation. The obtained results are highly relevant as they improve the interpretation of drug release kinetics from LUVs under osmotic stress. Moreover, the findings can be utilized in the development of liposomal formulations intended for nose-to-brain targeted drug delivery.

Objective: Development of liposomal mucoadhesive drug delivery system, which is able to improve the bioavailability of poorly absorbed oral drugs by prolonging their gastric and intestinal residence time, through facilitating the intimate contact of the delivery system with the absorption membrane. Materials and methods: Liposomes containing model drug atenolol were prepared by the modified ethanol injection method. Liposomes containing atenolol were coated by different mucoadhesive polymers, for example, chitosan, Carbopol 974P, Eudragit L100, and Eudragit S100, to optimize the choice of coating material. The delivery systems were tested for their in vitro mucoadhesiveness. Results: Liposomes prepared by the ethanol injection method were of satisfactory size (around 100 nm, before coating). Through the coating of liposomes in the presence of unentrapped material, the entrapment efficiency for drug was increased. In vitro mucoadhesive test confirmed the mucoadhesive properties of the coated layer for all tested polymers; however, Eudragit S100-coated liposomes were superior to other coating materials. Discussion: Eudragit coating appeared to be an optimal polymer choice. These preliminary data indicate that polymer-coated mucoadhesive liposomes are able to carry sufficient amount of drug and to remain attached to the intestinal mucosa for a sufficient period of time to enable prolonged absorption of entrapped drug. Conclusion: While keeping in mind that the in vivo conditions may vary with the in vitro ones, we may recommend the system described in our work for possible oral delivery of peptides and phytochemicals.