Medium and long-chain structured triacylglycerol enhance Vitamin D bioavailability in emulsion-based delivery system: a combination of in vitro and in vivo studies

2022 ◽  
Author(s):  
Yiwen Guo ◽  
Ying Xu ◽  
Tao Zhang ◽  
Yandan Wang ◽  
Ruijie Liu ◽  
...  

Vitamin D (VitD) is an essential fat-soluble micronutrient required for maintaining and regulating calcium homeostasis. Although sunlight can provide VitD, epidemiological studies indicate that VitD deficiency and insufficiency are widespread....

2021 ◽  
Vol 18 ◽  
Author(s):  
Subheet Kumar Jain ◽  
Neha Panchal ◽  
Amrinder Singh ◽  
Shubham Thakur ◽  
Navid Reza Shahtaghi ◽  
...  

Background: Diclofenac sodium (DS) injection is widely used in the management of acute or chronic pain and inflammatory diseases. It incorporates 20 % w/v Transcutol-P as a solubilizer to make the stable injectable formulation. However, the use of Transcutol-P in high concentration leads to adverse effects such as severe nephrotoxicity, etc. Some advancements resulted in the formulation of an aqueous based injectable but that too used benzyl alcohol reported to be toxic for human use. Objective: To develop an injectable self-micro emulsifying drug delivery system (SMEDDS) as a novel carrier of DS for prompt release with better safety and efficacy. Methods: A solubility study was performed with different surfactants and co-surfactants. The conventional stirring method was employed for the formulation of SMEDDS. Detailed in vitro characterization was done for different quality control parameters. In vivo studies were performed using Wistar rats for pharmacokinetic evaluation, toxicological analysis, and analgesic activity. Results: The optimized formulation exhibited good physical stability, ideal globule size (156±0.4 nm), quick release, better therapeutics, and safety, increase in LD50 (221.9 mg/kg) to that of the commercial counterpart (109.9 mg/kg). Further, pre-treatment with optimized formulation reduced the carrageenan-induced rat paw oedema by 88±1.2 % after 4 h, compared to 77±1.6 % inhibition with commercial DS formulation. Moreover, optimized formulation significantly (p<0.05) inhibited the pain sensation in the acetic-acid induced writhing test in mice compared to its commercial equivalent with a better pharmacokinetic profile. Conclusion: The above findings confirmed that liquid SMEDDS could be a successful carrier for the safe and effective delivery of DS


2018 ◽  
Vol 62 (4) ◽  
pp. 1700836 ◽  
Author(s):  
Alagu Selvi Kadappan ◽  
Chi Guo ◽  
Cansu E. Gumus ◽  
Amy Bessey ◽  
Richard J. Wood ◽  
...  
Keyword(s):  

2013 ◽  
Vol 66 (5-6) ◽  
pp. 259-262
Author(s):  
Goran Marusic ◽  
Dimitrije Jeremic ◽  
Sasa Vojinov ◽  
Natasa Filipovic ◽  
Milan Popov

In addition to the metabolic role of vitamin D, which is well known and clearly defined, there have been many hypotheses regarding its anti-proliferative and pro-apoptotic role. Epidemiology and Significance of Prostate Cancer. Prostate cancer is the second most common malignancy in men. Long period of cancerogenesis, available tumor markers and high incidence make this cancer ideal for preventive measures. Physiological Role of Vitamin D and its Effect on Prostate Cancer Cells. In vitro and in vivo studies have shown the anti-proliferative and pro-apoptopic role of vitamin D. Disorders of vitamin D metabolism are noted in vitamin D gene level, vitamin D receptor, vitamin D responsive elements and androgen receptors. We present the most important effect of those changes on vitamin D metabolism. Conclusion. Available studies on vitamin D level in serum, prostate tissue, observed activity of vitamin D enzymes and genetic changes give us only a slight insight into the basic mechanisms of vitamin D action in the development of prostate cancer; therefore, further investigations are needed.


2007 ◽  
Vol 292 (5) ◽  
pp. F1390-F1395 ◽  
Author(s):  
M. E. Rodriguez ◽  
Y. Almaden ◽  
S. Cañadillas ◽  
A. Canalejo ◽  
E. Siendones ◽  
...  

We previously demonstrated that extracellular calcium regulates vitamin D receptor (VDR) expression by parathyroid cells. Since the calcimimetic R-568 potentiates the effects of calcium on the calcium-sensing receptor, it was hypothesized that administration of R-568 may result in increased VDR expression in parathyroid tissue. In vitro studies of the effect of R-568 on VDR mRNA and protein were conducted in cultures of whole rat parathyroid glands and human hyperplastic parathyroid glands. In vivo studies in Wistar rats examined the effect of R-568 and calcitriol alone and in combination. Incubation of rat parathyroid glands in vitro with R-568 (0.001–1 μM) resulted in a dose-dependent decrease in parathyroid hormone (PTH) secretion and an increase in VDR expression (mean ± SE). Incubation in 1 mM calcium + 0.001 μM R-568 elicited an increase in VDR mRNA (306 ± 46%) similar to the maximum increase detected with 1.5 mM calcium (330 ± 42%). In vivo, VDR mRNA was increased after administration of R-568 (168 ± 9%, P < 0.001 vs. control) or calcitriol (198 ± 16%, P < 0.001 vs. control). Treatment with R-568 also increased VDR protein in normal rat parathyroid glands and in human parathyroid glands with diffuse, but not nodular, hyperplasia. In conclusion, the present study shows that the calcimimetic R-568 exerts a stimulatory effect on VDR expression in the parathyroid glands of study models and provides additional evidence for the use of calcimimetics in the treatment of secondary hyperparathyroidism.


Foods ◽  
2019 ◽  
Vol 8 (10) ◽  
pp. 474 ◽  
Author(s):  
Domenico Cautela ◽  
Filomena Monica Vella ◽  
Bruna Laratta

Experimental and epidemiological studies show a positive relation between consumption of citrus juices and reduction of risk for some chronic disorders, such as diabetes and cardiovascular diseases. In particular, the bergamot juice is characterized by noticeable amounts of phytochemicals such as flavanone glycosides, limonoids, and quaternary ammonium compounds, all health-beneficial biomolecules. In vitro and in vivo studies have shown anti-inflammatory, cholesterol-lowering, and anti-diabetic activities attributed to these compounds depending on their chemical structure. However, nutritional content of bergamot juice may vary as consequence of different processing techniques, thus needing to address this claim. For this reason, the objective of this research was to evaluate the effects of different processing systems on the proximate constituents, the composition, and the antioxidant activity of the correspondent juices. Overall, the results indicate that the process employed may influence the chemical composition and the functional properties of the ended juice. Screw press method produced a juice with greater content of flavanone glycosides (ranged from 37 to 402 mg/L) and limonoid aglycones (ranged from 65 to 67 mg/L) than the other processes (p < 0.001). However, the process used for extraction of bergamot juice did not affect significantly the N,N-dimethyl-L-proline content (p < 0.5). Moreover, the screw press juice showed the highest antioxidant activity with EC50 value of 9.35 µg/mL, thus suggesting that this method maintains for health the nutritional quality of a fresh-pressed juice.


2001 ◽  
pp. 129-134 ◽  
Author(s):  
P This ◽  
A De La Rochefordi√®re ◽  
K Clough ◽  
A Fourquet ◽  
H Magdelenat ◽  
...  

The current extension of the indications for adjuvant chemotherapy, which predisposes to early menopause, and the media coverage of the benefits of hormone replacement therapy (HRT) have led patients with a history of breast cancer to seek treatments for estrogen deprivation. In breast cancer survivors, most physicians avoid HRT because of concern regarding the potential promotion of growth of occult malignant cells by estrogens, due to the estrogen dependence of breast cancer. Soy phytoestrogens are being promoted as the 'natural alternative' to HRT and have been available without restrictions for several years as nutritional supplements. In this paper, data on the complex mammary effects of phytoestrogens in epidemiological studies, in in vitro studies, as well as in in vivo studies on animal carcinogenesis are reviewed. The potential benefits and risks of phytoestrogens are analyzed, and the prescription of phytoestrogens to postmenopausal women after breast cancer and the coprescription with the anti-estrogen tamoxifen are discussed. The absence of controlled trials and technical checking of extraction and titration in these preparations on 'free sale' raise a new problem in terms of public health and justify close reasoning and a cautious attitude of physicians, as well as straight information given to women, especially after breast cancer.


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