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Dramatic Improvement of Facial Angiofibromas in Tuberous Sclerosis With Topical Rapamycin: Optimizing a Treatment Protocol

Dramatic Improvement of Facial Angiofibromas in Tuberous Sclerosis With Topical Rapamycin:... In a recent report on the use of topical rapamycin to treat facial angiofibromas, Haemel et al1 demonstrated the efficacy of rapamycin tablets mixed in petrolatum, 1%, ointment. Based on these findings and another report of topical rapamycin solution compounded with Eucerin (Eucerin, Hamburg, Germany),2 we proceeded with a similar approach in our patient with tuberous sclerosis complex (TSC). We encountered several difficulties in creating a well-tolerated formulation of topical rapamycin. It is well known that liquid rapamycin cannot be compounded into 1% ointment because it forms an unstable emulsion. Therefore, our initial compound consisted of rapamycin tablets that were first dissolved in alcohol, to remove the hard coating, and then compounded in petrolatum. Within the first few days of use, this compound caused burning and an irritant dermatitis, which we attributed to the alcohol. A compounding attempt without alcohol produced a gritty, abrasive paste. Finally, an elegant formulation was achieved without alcohol by a compounding process involving 5 steps: Crush 300 2-mg tablets in a pharmaceutical blender; do not use a mortar and pestle because the tablets have a hard coating. Sift the powder through a mesh to remove large parts of the inactive coating. Wet the powder with a small amount of mineral oil to make a thick paste. Mix in white petrolatum for a total of 60 g, first by hand and then in an Unguator (GAKO International GmbH, Munich, Germany) or similar machine. Repeat blending (3 times) in an ointment mill. The final product of topical rapamycin, 1%, is cosmetically appealing and very well tolerated. After applying topical rapamycin, 1%, twice daily for a month, using 1.0 g per dose, our patient improved dramatically (Figure). We recommend this rapamycin, 1%, compound applied twice daily to treat facial angiofibromas. View LargeDownload Figure. Facial angiofibromas before (A) and after (B) treatment with topical rapamycin, 1%. Our case confirms the efficacy of topical rapamycin in diminishing facial angiofibromas. Our challenges in producing an elegant formulation can direct a future protocol for optimizing treatment of facial angiofibromas in patients with TSC using topical rapamycin. Back to top Article Information Correspondence: Dr DeKlotz, Division of Dermatology, Department of Medicine, Georgetown University Hospital/Washington Hospital Center, 5530 Wisconsin Ave, Ste 730, Chevy Chase, MD 20815 (cyndee.carver@gmail.com). Financial Disclosure: None reported Additional Contributions: Greg Chase, RPh, and Frank Odeh, RPh, provided guidance and collaboration in the compounding process. References 1. Haemel AK, O ’Brian AL, Teng JM. Topical rapamycin: a novel approach to facial angiofibromas in tuberous sclerosis. Arch Dermatol. 2010;146(7):715-71820644030PubMedGoogle ScholarCrossref 2. McNamara EK, Curtis AR, Fleischer AB. Successful treatment of angiofibromata of tuberous sclerosis complex with rapamycin [published online August 1, 2010]. J Dermatolog Treat20673154PubMedGoogle Scholar http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Archives of Dermatology American Medical Association

Dramatic Improvement of Facial Angiofibromas in Tuberous Sclerosis With Topical Rapamycin: Optimizing a Treatment Protocol

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Publisher
American Medical Association
Copyright
Copyright © 2011 American Medical Association. All Rights Reserved.
ISSN
0003-987X
eISSN
1538-3652
DOI
10.1001/archdermatol.2011.254
Publisher site
See Article on Publisher Site

Abstract

In a recent report on the use of topical rapamycin to treat facial angiofibromas, Haemel et al1 demonstrated the efficacy of rapamycin tablets mixed in petrolatum, 1%, ointment. Based on these findings and another report of topical rapamycin solution compounded with Eucerin (Eucerin, Hamburg, Germany),2 we proceeded with a similar approach in our patient with tuberous sclerosis complex (TSC). We encountered several difficulties in creating a well-tolerated formulation of topical rapamycin. It is well known that liquid rapamycin cannot be compounded into 1% ointment because it forms an unstable emulsion. Therefore, our initial compound consisted of rapamycin tablets that were first dissolved in alcohol, to remove the hard coating, and then compounded in petrolatum. Within the first few days of use, this compound caused burning and an irritant dermatitis, which we attributed to the alcohol. A compounding attempt without alcohol produced a gritty, abrasive paste. Finally, an elegant formulation was achieved without alcohol by a compounding process involving 5 steps: Crush 300 2-mg tablets in a pharmaceutical blender; do not use a mortar and pestle because the tablets have a hard coating. Sift the powder through a mesh to remove large parts of the inactive coating. Wet the powder with a small amount of mineral oil to make a thick paste. Mix in white petrolatum for a total of 60 g, first by hand and then in an Unguator (GAKO International GmbH, Munich, Germany) or similar machine. Repeat blending (3 times) in an ointment mill. The final product of topical rapamycin, 1%, is cosmetically appealing and very well tolerated. After applying topical rapamycin, 1%, twice daily for a month, using 1.0 g per dose, our patient improved dramatically (Figure). We recommend this rapamycin, 1%, compound applied twice daily to treat facial angiofibromas. View LargeDownload Figure. Facial angiofibromas before (A) and after (B) treatment with topical rapamycin, 1%. Our case confirms the efficacy of topical rapamycin in diminishing facial angiofibromas. Our challenges in producing an elegant formulation can direct a future protocol for optimizing treatment of facial angiofibromas in patients with TSC using topical rapamycin. Back to top Article Information Correspondence: Dr DeKlotz, Division of Dermatology, Department of Medicine, Georgetown University Hospital/Washington Hospital Center, 5530 Wisconsin Ave, Ste 730, Chevy Chase, MD 20815 (cyndee.carver@gmail.com). Financial Disclosure: None reported Additional Contributions: Greg Chase, RPh, and Frank Odeh, RPh, provided guidance and collaboration in the compounding process. References 1. Haemel AK, O ’Brian AL, Teng JM. Topical rapamycin: a novel approach to facial angiofibromas in tuberous sclerosis. Arch Dermatol. 2010;146(7):715-71820644030PubMedGoogle ScholarCrossref 2. McNamara EK, Curtis AR, Fleischer AB. Successful treatment of angiofibromata of tuberous sclerosis complex with rapamycin [published online August 1, 2010]. J Dermatolog Treat20673154PubMedGoogle Scholar

Journal

Archives of DermatologyAmerican Medical Association

Published: Sep 1, 2011

Keywords: rapamycin,angiofibroma,face,tuberous sclerosis

References