Long-term stability of 0.1% rapamycin hydrophilic gel in the treatment of facial angiofibromas.
Administration, Topical
Angiofibroma
/ drug therapy
Antibiotics, Antineoplastic
/ administration & dosage
Chromatography, High Pressure Liquid
/ methods
Drug Compounding
/ methods
Drug Stability
Facial Neoplasms
/ drug therapy
Gels
Humans
Hydrophobic and Hydrophilic Interactions
Sirolimus
/ administration & dosage
Treatment Outcome
angiofibromas
hydrophilic gel
rapamycin
stability
topical formulation
tuberous sclerosis
Journal
European journal of hospital pharmacy : science and practice
ISSN: 2047-9956
Titre abrégé: Eur J Hosp Pharm
Pays: England
ID NLM: 101578294
Informations de publication
Date de publication:
03 2020
03 2020
Historique:
received:
25
07
2018
revised:
04
10
2018
accepted:
09
10
2018
entrez:
17
4
2020
pubmed:
17
4
2020
medline:
10
8
2021
Statut:
ppublish
Résumé
In recent years, various formulations containing rapamycin, mainly petrolatum-based, have been tested on facial angiofibromas in tuberous sclerosis. They are often poorly tolerated due to irritation and bleeding. In addition, their effectiveness was insufficient in young adults. The objective of this study was to develop and characterise a hydro-alcoholic gel containing solubilised rapamycin. The stability of the product stored at 4°C was evaluated over 1 year. Two different 0.1% rapamycin gels were formulated with or without α-tocopherol and urea. Different methods were used to characterise the gels: HPLC, gas chromatography, pH, visual observation and optical microscopy. A physico-chemical and microbiological stability study was also conducted for 1 year at 4°C. Gels were physically and microbiologically stable after 1 year at 4°C: organoleptic characteristics and pH unchanged, no significant decrease in rapamycin was observed, tocopherol droplet size was constant and rheological behaviour was not altered. This study describes a new gel formulation to improve skin penetration using various excipients to promote skin tolerance. This study provides, for the first time, detailed stability data for a hydro-alcoholic rapamycin gel.
Identifiants
pubmed: 32296505
doi: 10.1136/ejhpharm-2018-001695
pii: ejhpharm-2018-001695
pmc: PMC7147563
doi:
Substances chimiques
Antibiotics, Antineoplastic
0
Gels
0
Sirolimus
W36ZG6FT64
Types de publication
Journal Article
Langues
eng
Pagination
e48-e52Informations de copyright
© European Association of Hospital Pharmacists 2020. No commercial re-use. See rights and permissions. Published by BMJ.
Déclaration de conflit d'intérêts
Competing interests: None declared.
Références
Arch Dermatol. 2011 Sep;147(9):1116-7
pubmed: 21931059
J Am Acad Dermatol. 2017 Sep;77(3):464-472.e3
pubmed: 28502378
Dermatology. 2018;234(1-2):13-22
pubmed: 29925060
Australas J Dermatol. 2012 Feb;53(1):52-6
pubmed: 22309333
Br J Dermatol. 2008 Jul;159(1):23-34
pubmed: 18510666
Proc Natl Acad Sci U S A. 2003 Jun 10;100(12):7360-5
pubmed: 12771381
Adv Drug Deliv Rev. 2004 Mar 27;56(5):603-18
pubmed: 15019749
Australas J Dermatol. 2014 Feb;55(1):63-9
pubmed: 24359523
Br J Dermatol. 2011 Oct;165(4):922-3
pubmed: 21692776
J Mol Med (Berl). 1995 Jan;73(1):7-17
pubmed: 7633944
Drugs R D. 2012 Sep 1;12(3):121-6
pubmed: 22934754
JAMA Dermatol. 2017 Jan 1;153(1):39-48
pubmed: 27837201
Br J Dermatol. 2013 Dec;169(6):1314-8
pubmed: 23909960
J Antibiot (Tokyo). 1975 Oct;28(10):721-6
pubmed: 1102508
J Child Neurol. 2013 Jul;28(7):933-6
pubmed: 23680945
Pediatr Dermatol. 2016 Sep;33(5):518-25
pubmed: 27436143
Proc Natl Acad Sci U S A. 2008 Mar 4;105(9):3539-44
pubmed: 18292222
J Drugs Dermatol. 2016 May 1;15(5):633-9
pubmed: 27168272
Int J Pharm. 2016 Jul 25;509(1-2):279-284
pubmed: 27260135
Arch Dermatol. 2010 Jul;146(7):715-8
pubmed: 20644030
J Eur Acad Dermatol Venereol. 2012 Oct;26(10):1315-8
pubmed: 21834948
J Am Acad Dermatol. 2004 Jul;51(1 Suppl):S9-11
pubmed: 15243489