Assessing compatibility of excipients selected for a sustained release formulation of bilberry leaf extract

Abstract The study is aimed to assess the compatibility of bilberry leaf powder extract (BLPE) with six excipients selected for sustained-release (SR) tablet formulation. The BLPE was obtained with the addition of L-arginine and Myo-inositol as the carriers. Thermogravimetric (TG-DTG) analysis and Fourier-transform infrared spectroscopy (FTIR), supported by Pearson correlation analysis, were applied to detect possible interactions in the binary mixtures (1:1) of the BLPE with each excipient. The TG-DTG showed some deviations in the thermal behavior of the BLPE / excipient mixtures. However, only the thermal behavior of magnesium stearate in the mixture significantly differed from individual samples, which suggested chemical interaction for this excipient. The FTIR analysis confirmed that the BLPE is compatible with Eudragit L100, Methocel K4M, Methocel K100LV, Avicel PH-101, and Plasdone S-630. Whereas it undergoes solid-state chemical interaction in the binary mixture with magnesium stearate. According to the FTIR-spectra, it is suggested that this interaction results in the formation of stearic acid and alkalization of the medium. These findings evidence for the possibility of using TG-DTG analysis as an independent thermal technique for compatibility studies and also confirm the earlier reported interaction of basic lubricants, e.g., stearic salts, with active ingredients containing amino groups.

Bilberry Products: Modern Characterization of Commercial Extracts / 日本補完代替医療学会誌

Wild north European bilberry (Vaccinium myrtillus) is one of the richest botanical sources of anthocyanins, a class of molecules responsible for the color of fruits and characterized by a strong antioxidant activity.From a biological point of view, anthocyanins are endowed with several diverse activities and high quality bilberry extracts have been clinically studied in conditions like chronic venous insufficiency and diabetic retinopathy.Given the complexity of the industrial bilberries supply chain and thereof the high cost of their anthocyanins rich extracts, the dietary supplements market is facing a dramatic presence of adulterated extracts, either due to the use of anthocyanins from cheaper sources not related to bilberry or of chemical dyes.Although the current landscape is quite challenging, methods to detect the adulterations are at hand and need to be routinely implemented along the supply chain up to the finished product on the shelf.This review summarizes the market situation and gives a picture of the most recent analytical techniques available to the industry in order to spot these counterfeits and guarantee to the consumers a better quality and consistence of the products.

Effects of Bilberry on Deoxyribonucleic Acid Damage and Oxidant-Antioxidant Balance in the Lens, Induced by Ultraviolet Radiation

Background: This study investigated the possible protective effects of bilberry extract after exposing rat eyes to ultraviolet-B (UV-B) radiation. Methods: Four groups of rats were included in this study, each consisting of 10 Wistar rats. The first group acted as the control, and the second group was exposed to UV-B, 5 KJ/m2 (λm = 300 nm), for 15 minutes. The third group was orally administered bilberry extract (160 mg twice per day) for two weeks before exposure to the UV-B, while the fourth group was administered the same dose of bilberry extract for two weeks before euthanisation. A comet assay was used to examine DNA damage, while the malondialdehyde (MDA) level and superoxide dismutase (SOD), glutathione peroxidase (GSH-Px) and catalase (CAT), activities were measured in the lens. Results: After exposing the rats to UV-B radiation, the mean percentage tail DNA and tail moment were significantly increased (P < 0.001) when compared to the control group. In the same context, the lens tissue MDA levels and CAT activity were also significantly increased (P < 0.001). The supplementation of the bilberry extract was found to improve the comet assay parameters and enzymatic activity of the rat lens tissue. Conclusion: The administration of bilberry led to a decrease in the oxidative stress in the lens tissues and DNA damage induced by UV-B radiation in the lenses of Wistar rats.

The Efficacy of Vaccinium Uliginosum for Early Age-Related Macula Degeneration

PURPOSE: To evaluate the effect of Bog Bilberry (Vaccinium uliginosum) extract in eyes with early age-related macular degeneration (AMD). METHODS: Forty-four eyes of forty four patients with early AMD were included in this randomized, double-blinded, and placebo-controlled study. All participants were randomly assigned to either the placebo group (n = 24), or the bog bilberry extract group (n = 20). Before drug administration, an ophthalmic examination which included slit lamp microscopy, best corrected visual acuity, and intraocular pressure was performed, and repeated 1and 3 months after treatment. Objective scatter index, glare and tear film break-up time were checked by Optical Quality Analysis System (OQAS, Visiometrics, Spain) and drusen volume, central macular thickness, and RPE and IS/OS junction thickness were investigated with spectral-domain optical coherence tomography (Spectralis, Heidelberg, Germany). RESULTS: In the bog bilberry extract group, RPE and IS/OS junction thickness was significantly increased compared to the placebo group after 3 months of drug administration. CONCLUSIONS: Bog Bilberry extract may play a favorable role in preventing the atrophic change of RPE and IS/OS junction layer and the progression of early macular degeneration.

Bilberry extract induces apoptosis of Hela cells and its action mechanism / 医学研究生学报

Objective: Bilberry extract can inhibit the growth of cancer cells,but its effect on cervical carcinoma is rarely reported.This study was to explore the effects of bilberry extract on the expressions of Bcl-2,Bax,Fas and FasL in Hela cells.Methods: We determined the apoptosis of Hela cells by Hoechst33342/PI fluorescent staining and DNA ladder and Annexin V/PI double-staining after exposed to bilberry extract at the concentrations of 0.025-25 ?g/ml for 24 hours,and the protein expressions of Bcl-2,Bax,Fas and FasL were detected by Western blotting.Results: Obvious apoptosis-associated morphological changes and specific DNA ladder bands were observed in the Hela cells after exposed to bilberry extract at the concentrations of 0.025,0.25,2.5 and 25 ?g/ml,and the apoptosis rates of the cells were(4.13 ? 0.63)%,(5.41 ? 0.77)%,(8.74 ? 1.27)% and(12.05 ? 1.03)%,respectively.Western blot showed increased expressions of bax,Fas and FasL,and a decreased expression of bcl-2.Conclusion: Bilberry extract induces the apoptosis of Hela cells by up-regulating the protein expressions bax,Fas and FasL and down-regulating that of bcl-2.