Studies on cyclodextrin polymer. Part 1: The effect of CDP on indomethacin tablet formulation.

Cyclodextrin polymer (CDP), which is a cross-linked derivative of beta-cyclodextrin, has been used as binder and disintegrating agent in tablet formulation. In this study different tablet formulations of indomethacin, which is a nonsteroid anti-inflammatory drug were prepared by direct compression method. Corn starch, lactose and Esma-Spreng were used besides CDP as disintegrating agent. The hardness, friability, disintegration time and dissolution rate of the tablet were determined. The data were also evaluated kinetically. It was found that CDP is a good disintegrating agent and significantly increased the dissolution rate of the poorly soluble indomethacin.

Effects of polyphenols on skin damage due to ultraviolet A rays: an experimental study on rats.

BACKGROUND: Ultraviolet (UV) radiation causes many acute and chronic conditions such as oedema of the skin, sunburn, immunosuppression, photo-ageing and skin cancer. The use of antioxidants has become of paramount importance in prevention of the damage caused by ultraviolet radiation. Epigallocatechin-3-gallate (EGCG), one of the main components of green tea, has been reported to have anti-inflammatory, antioxidant and anticarcinogenic properties. AIM: The aim of this experimental study was to investigate to what extent EGCG prevented acute skin damage caused by UVA. MATERIAL AND METHOD: The sample contained 2% EGCG, which was prepared in hydrophilic ointment (USP XXIV) as the vehicle. Twenty-four 12-week-old Wistar albino rats are included in the study and divided into four groups, each containing six rats. Group I was formed to be the control group, which was not applied any topical medication or exposed to UV radiation. Group II was formed to observe acute effects of UVA on the skin, Group III was formed to observe effectiveness of topical EGCG on the skin applied 30 min after exposure to UVA, and Group IV was formed to observe topical EGCG applied 30 min before exposure to UVA. All groups were examined for sunburn cells, leucocyte infiltration, dermo-epidermal activity, collagen changes and elastic fibre pathologies on 24 and 72 h. Statistical analysis was performed using spss 11.5, and chi-squared test was used for the evaluation of parameters. RESULTS: Group IV showed a statistically significant decrease in sunburn cells and dermo-epidermal activation compared with Group II. Group II showed significant increase in all parameters compared with Group I, showing the effects of UV exposure alone, and no difference was detected in Group II and III. CONCLUSION: These results show a protective effect of EGCG when applied topically before UVA exposure. No benefit was detected when EGCG was applied after UV exposure.

Improved efficacy and tolerability of retinoic acid in acne vulgaris: a new topical formulation with cyclodextrin complex psi.

OBJECTIVES: Retinoic acid (RA) has long been used, both topically and systemically, for disorders of keratinization, acne and related disorders. In the present study, the efficacy and tolerability of topical RA prepared as a cyclodextrin beta complex (beta-CD) is investigated in 66 acne vulgaris patients. METHODS: This randomized, double-blind, placebo-controlled study compares nightly topical application of RA/beta-CD complex hydrogel formulation (0.025%), RA/beta-CD complex in moisturizing base (0.025%), hydrogel base, moisturizer base or a commercial RA gel (0.05%) in acne vulgaris patients. Improvement of acne was assessed using a 5-point improvement scale and by measuring sebum and moisture content of the skin using an SM 810 sebumeter/corneometer. RESULTS: After 3 months of treatment, mean scores of acne improvement on the 5-point scale were 4 with the RA/beta-CD complex hydrogel formulation, 4.1 with the RA/beta-CD complex in moisturizing base, 1.2 with hydrogel placebo base, 1.1 with moisturizer placebo base and 3 with the commercial RA product. All patients treated with the commercial product experienced local side-effects. One patient discontinued due to severe irritation. None of the patients treated with the RA/beta-CD complex in the moisturizing base and hydrogel formulation experienced significant local irritation, although the sebum content of the skin decreased after application of the RA/beta-CD preparations. This change was not significant compared to controls. The moisture content of the skin was better preserved in the group treated with the RA/beta-CD complex in the moisturizing base. CONCLUSION: The topical RA/beta-CD complex, in hydrogel and moisturizing base, was more effective than the twice concentrated commercial RA product. There were few topical side-effects with this new formulation, which increases patient compliance. Topical RA/beta-CD (0.025% RA) did not significantly reduce sebum secretion but may help to preserve optimum epidermal moisture content with the proper base formulation. This is the first study in the literature reporting efficacy and tolerability of the topical RA/beta-CD complex in acne vulgaris. We conclude that the topical RA/beta-CD complex displays an improved efficacy and tolerability profile and is an effective treatment alternative for acne vulgaris.