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Pimecrolimus
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Contact allergy to the excipient oleyl alcohol in the commercial pimecrolimus cream has been described (6). This cream also contains the well-known sensitizer propylene glycol (PG), but in patients allergic to PG, pimecrolimus cream showed a very low potential to elicit allergic skin reactions (8). In one case, a patient had a positive patch test to the commercial cream but not to any of its ingredients (7).
Oils
Published in Heather A.E. Benson, Michael S. Roberts, Vânia Rodrigues Leite-Silva, Kenneth A. Walters, Cosmetic Formulation, 2019
Fabricio Almeida de Sousa, Vânia Rodrigues Leite-Silva
Esters are the product of the reaction of any acid (usually organic) and alcohol. Common fatty acids are caprylic, capric, lauric, myristic, palmitic, stearic, oleic, linoleic and behenic acids, and dicarboxilic acids such as adipic acid. Common alcohols are isopropyl, n-butyl, ethylhexyl, myristyl or oleyl alcohol, as well as polyvalent alcohols such as ethylene glycol, polyglycerol, propylene glycol and glycerol. A wide range of combinations can be used to produce the large range of synthetic esters available to the cosmetic industry.
Chemical Modulation of Topical and Transdermal Permeation
Published in Marc B. Brown, Adrian C. Williams, The Art and Science of Dermal Formulation Development, 2019
Marc B. Brown, Adrian C. Williams
Fatty alcohols (also termed “alkanols”) are typically applied in a co-solvent (for example, propylene glycol), at between 1 and 10%. As with the fatty acids (Section 3.2.2.5), some structure/activity relationships for fatty alcohol penetration enhancement have shown lower activities for branched alkanols compared to linear molecules. For saturated fatty alcohols, efficacy tends to increase up to ~C10 and then falls as chain length increases further. As with the fatty acids, enhancement efficacy generally increases with the inclusion of up to two unsaturated bonds into the alcohols, again likely due to the formation of free volume within the intercellular lipid bilayers as the fatty alcohol intercalates into their structure. Oleyl alcohol (cis-9-octadecen-1-ol) is an unsaturated fatty alcohol that functions as a non-ionic surfactant and which has been widely used as a chemical penetration enhancer.
Alternative method to improve the ethyl valerate yield using an immobilised Burkholderia cepacia lipase
Published in Journal of Microencapsulation, 2019
Wellington Correa Moreira, Alfredo Luís Pereira Elias, Wislei Riuper Osório, Giovana Silva Padilha
In this present investigation, the results obtained are agreed with those previously reported by Lau et al. (2014) (Lau et al. 2014), where a commercial Lipozyme and Novozym 435 in the esterification of the lauric acid and oleyl alcohol is applied. Based on the previous reports, 10g of Novozym 435 and 10g of Lipozyme have their costs of about ∼ US$200 (Mahapatra et al. 2009) and US$400 (Lau et al. 2014), respectively. It can be seen that Burkholderia cepacia lipase is of about 7 and 12 times cheaper (∼ US$40 per 10g) (Sigma Aldrich 2018) than other two lipases, respectively. Also, this is associated with the fact that their immobilisation into an alginate medium also indicates a cheaper alternative for a good esterification yield of the ethyl valerate.
Development and evaluation of a drug-in-adhesive transdermal delivery system for delivery of olanzapine
Published in Expert Opinion on Drug Delivery, 2022
Olanzapine was purchased from TCI America (Portland, OR), Pressure-sensitive adhesives (Acrylate DURO-TAK 87-2516 PSA and Polyisobutylene DURO-TAK 87-6908 PSA) were received as gift samples from Henkel Corporation (Dusseldorf, Germany), and Silicone BIO-PSA 7-4301 was received as a gift sample from Dow Corning Corporation (Washington, DC, USA). The release liners and backing membranes were gifted by 3M (St. Paul, MN, USA). Oleic acid, oleyl alcohol, and isopropyl alcohol were received as samples from Croda Inc. (Edison, NJ, USA). De-identified dermatomed human skin was procured from a New York Fire Fighters (New York, NY, USA), while dermatomed porcine skin was excised from porcine ears procured from a local slaughterhouse (Atlanta, GA, USA).
In vitro characterization of tofacitinib loaded novel nanoemulgel for topical delivery for the management of rheumatic arthritis
Published in Drug Development and Industrial Pharmacy, 2022
Suchitra Nishal, Vikas Jhawat, Parmita Phaugat, Rohit Dutt
Rheumatoid arthritis is an autoimmune disorder that is elicited by several cytokines and causes inflammation, pain, and stiffening of joints alongside bone destruction. The kinase lineages associated with rheumatoid arthritis are Janus kinase (JAK), p38 (mitogen activated protein kinase), and Syk (spleen tyrosine kinase). JAKs mainly transmit the signals from cytokines to the STATs (signal transducers and activators of transcription) which will induce proinflammatory cellular responses [6]. Disruption in JAK signaling can also provoke the development of rheumatoid arthritis. For the prevention and cure of rheumatoid arthritis, medicinal agents belonging to diverse categories like DMARDs (disease modifying anti-rheumatic drugs), NSAIDs (non-steroidal anti-inflammatory drugs), corticosteroids, antioxidants, and biologics are employed. JAK inhibitors are the modern medicinal agents exercised for the treatment of rheumatoid arthritis. Tofacitinib (TFB) is the pioneer JAK inhibitor possessing specific action for JAK1 and 3 with slight inhibitory action on Tyk2 (Tyrosine kinase) and JAK2 [7]. Oral administration of TFB is capable of restraining the signaling of various cytokines. TFB with 5 and 10 mg b.i.d. doses is effective in the management of rheumatoid arthritis; further, it shows its effectiveness in both individual as well as combined therapy with methotrexate and other DMARDs. Despite, the favorable impacts of oral TFB, discrete undesirable effects have been observed like increased chances of infections, upper respiratory infections, leukopenia, anemia, herpes zoster, cardiovascular diseases, etc. Consequently, attempts are being made to develop a topical formulation of TFB. Topical delivery of TFB may avoid the incidence of unpleasant effects; further, it possesses the requisites for topical formulation for example, low dose, low molecular weight, short half-life, etc. So far, TFB has not been used topically for rheumatoid arthritis however, for the treatment of other diseases like alopecia, and psoriasis its topical formulations have been prepared. Progress in the development of topical formulations of TFB needs more expansion. Previously, 2% ointment of TFB has been studied for cutaneous sarcoidosis [8,9]. Topical ointment formulation of TFB as free base has been developed, as described in US Patent No. 20120258976, which showed that an ointment of TFB based on PEG and 1.8% oleyl alcohol exhibited a significant increase in flux and cumulative permeation [10]. Furthermore, a US patent (16/254,0762019) revealed a topical TFB formulation prepared without ethyl alcohol using DMSO. Upon comparison to the amount of TFB in the systemic circulation, it showed the largest amount of TFB conserved in the skin [11]. For transdermal administration of TFB citrate proposomes, i.e. propylene glycol based liposomes have been employed. The combination of propylene glycol and soya phosphatidyl choline resulted in higher penetration of TFB citrate through the skin [12]. In the present study, attempts were made to develop a novel topical formulation of TFB with increased skin penetration for the treatment of rheumatoid arthritis. In contrast to ointments, NEGs are free from stickiness, stable, possess better patient compliance.