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Retinol
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Retinol or vitamin A is a fat-soluble vitamin that plays a vital role in vision, epithelial differentiation, growth, reproduction, pattern formation during embryogenesis, bone development, hematopoiesis, brain development and modulation of immune function. Dietary retinol is derived from a variety of carotenoids found in plants. It is enriched in the liver, egg yolks, and the fat component of dairy products. Pharmaceutical retinol is indicated for the treatment of vitamin A deficiency. In cosmetics, retinol may be present as skin conditioning agent (1). In pharmaceutical products, retinol is mostly employed as retinyl palmitate (Chapter 3.301) or retinyl acetate (CAS number127-47-9, EC number 204-844-2, molecular formula C22H32O2).
Fat-Soluble Vitamins
Published in Luke R. Bucci, Nutrition Applied to Injury Rehabilitation and Sports Medicine, 2020
This quote is presented to illustrate just one of the many essential roles vitamin A plays in the musculoskeletal system. Vitamin A was probably the first vitamin discovered, by McCollum and Davis, in 1915.477 Several recent reviews give a substantial amount of background information on the many vital roles and functions of the first vitamin.170,476–481 Confusion over the identity of vitamin A is common, due to the multiplicity of forms found in nature with vitamin A activity. In this chapter, vitamin A is retinol, with commercially available forms including all-trans-retinyl palmitate, all-trans-retinyl acetate, and retinol. Retinol and its derivatives are referred to as preformed vitamin A to distinguish retinoids from carotenoids. Over 500 carotenoids are known to exist,477–479 but by far the most important is β-carotene, which is actually two retinols combined with the alcohol groups removed.477–481 By itself, β-carotene is primarily an antioxidant, by virtue of its scavenging effects against singlet oxygen.482,483 However, upon demand, β-carotene is cleaved into two retinol molecules. Thus, β-carotene can supply retinol equivalents when preformed vitamin A is not available or insufficient to meet needs. This book will make a distinction between retinols and carotenoids, since their actions differ, although recognizing that some β-carotene can convert into retinol.
Interleukins and Metalloproteinases in Arthritis
Published in Thomas F. Kresina, Monoclonal Antibodies, Cytokines, and Arthritis, 2020
Interestingly, retinoic acid has been reported to induce the cellular release of IL-1 and phenanthroline and cycloheximide also inhibit the IL-1-induced cartilage autolysis (66). In addition, retinyl acetate has recently been reported to induce arthritis in C3H-Avy mice (85).
Voretigene neparvovec-rzyl for the treatment of biallelic RPE65 mutation–associated retinal dystrophy
Published in Expert Opinion on Orphan Drugs, 2018
Stephen Russell, Jean Bennett, Albert M. Maguire, Katherine A. High
No pharmacologic treatment other than voretigene neparvovec-rzyl (VN) is currently available for IRDs, although adults with severe to profound RP with bare light or no light perception in both eyes have been granted humanitarian access to the Argus II Retinal Prosthesis System. Several RPE65 gene therapy trials, using various gene constructs, vector formulations, surgical procedures, and unilateral treatment, have demonstrated transitory improvements in retinal function from baseline, but the effects were of variable durability [8–14]. In addition, in phase 1b trials, transient increases from baseline in GVF have been demonstrated in some study subjects treated with oral 9-cis-retinyl acetate [15,16]. However, none of these approaches are in late stages of clinical development.
Pharmacotherapy of retinal disease with visual cycle modulators
Published in Expert Opinion on Pharmacotherapy, 2018
Rehan M. Hussain, Ninel Z. Gregori, Thomas A. Ciulla, Byron L. Lam
In a human Phase 1b trial (NCT01014052), 18 patients with RP caused by mutations in RPE65 (72%) or LRAT (28%) were given once-daily oral 9-cis-retinyl-acetate (also known as QLT091001 or zuretinol acetate – developed by Novelion Therapeutics) 40 mg/m2/day for 7 days and many were found to have improvement in visual field and best-corrected visual acuity (BCVA) [16]. In the RP patients, 8 of 18 (44%) patients showed a ≥20% increase and 4 of 18 (22%) showed a ≥40% increase in functional retinal area as measured by Goldmann visual fields (GVF). Twelve (67%) and 5 (28%) of 18 RP patients showed a ≥5 and ≥10 ETDRS letter score increase of visual acuity, respectively, in one or both eyes at 2 or more visits within 2 months of treatment. The specific genotypes (LRAT or RPE65) did not appear to affect how patients responded to the drug [16]. There were no detectable improvements observed on standard electroretinography (ERG), although this could be related to the preexisting level of degeneration [17–19].
Oral delivery of lycopene-loaded microemulsion for brain-targeting: preparation, characterization, pharmacokinetic evaluation and tissue distribution
Published in Drug Delivery, 2019
Yunliang Guo, Xuyan Mao, Jing Zhang, Peng Sun, Haiyang Wang, Yue Zhang, Yingjuan Ma, Song Xu, Renjun Lv, Xueping Liu
Lycopene (Batch No. KS170313, 98.06% purity) was purchased from Shaanxi Kingsci Biotechnology Co., Ltd. (Shaanxi, China). The internal standard retinyl acetate (98.4% purity) was obtained from Shanghai Huicheng Biological Technology Co., Ltd. (Shanghai, China). Tween 80 (polysorbate 80, injection grade) was acquired from Nanjing Well Chemical Co., Ltd. (Nanjing, China). Transcutol HP (designed for oral administration, 99.986% purity) was received as gratis sample from Gattefossé (Lyon, France) and polyethylene glycol 400 (PEG 400) was provided by Tianjin Dingshengxin Chemical Industry Co., Ltd. (Tianjin, China). (R)-(+)-Limonene (97% purity), olive oil, glycerol, butylated hydroxytoluene (BHT), ethyl acetate, anhydrous ethanol and hexane were all bought from Shanghai Macklin Biochemical Technology Co., Ltd. (Shanghai, China). Ethyl oleate and oleic acid were obtained from Tianjin Guangfu Fine Chemical Research Institute (Tianjin, China) and Damao Chemical Reagent Factory (Tianjin, China), respectively. Soybean oil (medical grade) was procured from Jiangxi Yipusheng Pharmaceutical Co., Ltd. (Jiangxi, China). Corn oil was supplied by Shanghai Yuanye Biological Technology Co., Ltd. (Shanghai, China). Deionized water was generated with an ELGA-Purelab water purification system (Model CLXXUVFM2; ELGA LabWater, High Wycombe, UK). The HPLC grade mobile phase components methanol and acetonitrile were from TEDIA Company, Inc. (Fairfield, OH, USA), while dichloromethane was from Tianjin Kemio Chemical Reagent Exploitation Center (Tianjin, China). The centrifugal ultrafilter (0.22 µm pore size) was purchased from Millipore (Bedford, MA, USA). All other reagents used in the study were of analytical grade.