Download in electronic PDF format for $25



Search the Complete Journal Archives

Evaluation of Percutaneous Absorption Performance for Human Female Sexual Steroids into Pentravan Cream

Author(s):  Polonini Hudson C,Brandão Marcos Antônio F,Ferreira Anderson O,Ramos Cristiano,Raposo Nádia R B

Issue:  Jul/Aug 2014 - Volume 18, Number 4
View All Articles in Issue

Abstract:  There is a lack of studies on Pentravan cream, a widespread transdermal vehicle which is used by compounding pharmacies. The purpose of this study was to evaluate this transdermal vehicle. The permeation performance for progesterone, estradiol, and estriol in formulations containing each of those drugs separately, as well as an association of estradiol + estriol (Biest), was evaluated regarding their compounding process and their potential biological application. An excised female human skin model was used to predict the permeation and the retention of the active compounds in every skin layer in lieu of conventional tape stripping. Progesterone was the drug with the highest permeation (37.02 mcg cm–2 at the end of the experiment). Estradiol and estriol in Biest had permeations approximately 4-fold lower (9.44 mcg cm–2 for estradiol-Biest and 14.02 mcg cm–2 for estriol-Biest), and the profiles of estradiol in Eemuls and in Biest were almost the same (9.46 mcg cm–2 for Eemuls). All permeations followed pseudofirst order kinetics. For progesterone, using the percentage of permeation by dose, one can infer that a patient using the 1-g emulsion dose released by the pump containing 50 mg of progesterone will have 38.4 mg of progesterone liberated into his bloodstream, gradually and continuously for 48 hours. The results indicate that the vehicle was able to provide percutaneous absorption rates compatible with and higher than clinical treatment needs. Using the same rationale, the Eemuls would deliver practically the entire amount of estradiol load per dose (1.0 mg), approximately 0.5 mg of estradiol per day. As for the Biest, the dosing used would deliver almost 0.5 mg estradiol/day and 2.0 mg estriol/ day. Thus, according to the results, human female sexual hormones incorporated in the oil-in-water vanishing cream base and applied topically are expected to exert their biological activities systemically with good efficacy due to their satisfactory permeation through human skin. However, one must take into account that a high quantity of drug was delivered. Thus, to avoid patient overdose, care has to be taken regarding the quantity of emulsion used.

Related Keywords: Hudson C. Polonini, PhD, Marcos Antônio F. Brandão, PhD, Anderson O. Ferreira, MSc, Cristiano Ramos, MD, Nádia R. B. Raposo, PhD, sex steroids, hormone replacement, women, topical preparations, transdermal absorption, percutaneous absorption, progesterone, estradiol, estriol, estrogen, Pentravan cream, oil-in-water vanishing cream, semisolid formulations, transdermal vehicle, human skin permeation, drug retention, semisolid dosage forms, dermal permeability, patient compliance, patient adherence, airless plunger pump dosage control

Related Categories: EXCIPIENTS, HRT, PEER-REVIEWED, DOSAGE FORMS/DRUG CARRIERS, ENDOCRINOLOGY/HORMONES/ MENOPAUSE/ANDROPAUSE

Printer-Friendly Version

Related Articles from IJPC
Title (Click for Abstract / Details) Author Issue Page View/Buy
Evaluation of Percutaneous Absorption Performance for Human Female Sexual Steroids into Pentravan Cream Polonini Hudson C, Brandão Marcos Antônio F, Ferreira Anderson O, Ramos Cristiano, Raposo Nádia R B Jul/Aug 2014 332-340 Buy
Veterinary Transdermal Medications: A to Z Davidson Gigi S Mar/Apr 2003 106 Buy
Orodispersible Films for Compounding Pharmacies Ferreira Anderson O, Brandão Marcos Antônio F, Raposo Francisco José, Polonini Hudson C, Raposo Nádia Rezende Barbosa Nov/Dec 2017 454-461 Buy
Stability of Allopurinol, Amitriptyline Hydrochloride, Carbamazepine, Domperidone, Isoniazid, Ketoconazole, Lisinopril, Naproxen, Paracetamol (Acetaminophen), and Sertraline Hydrochloride in SyrSpend SF PH4 Oral Suspensions Polonini Hudson C, Loures Sharlene, de Araujo Edson Peter, Brandão Marcos Antônio F, Ferreira Anderson O Sep/Oct 2016 426-434 Buy
Stability of Alprazolam, Atropine Sulfate, Glutamine, Levofloxacin, Metoprolol Tartrate, Nitrofurantoin, Ondansetron Hydrochloride, Oxandrolone, Pregabaline, and Riboflavin in SyrSpend SF pH4 Oral Suspensions de Oliveira Ferreira Anderson, Polonini Hudson C, Loures da Silva Sharlene, Cerqueira de Melo Victor Augusto, de Andrade Laura, Fernandes Brandão Marcos Antônio May/Jun 2017 255-263 Buy
Stability of Atenolol, Clonazepam, Dexamethasone, Diclofenac Sodium, Diltiazem, Enalapril Maleate, Ketoprofen, Lamotrigine, Penicillamine-D, and Thiamine in SyrSpend SF PH4 Oral Suspensions Polonini Hudson C, Loures Sharlene, Lima Luis Claudio, Ferreira Anderson O, Brandão Marcos Antônio F Mar/Apr 2016 167-174 Buy
Stability of Acetazolamide, Baclofen, Dipyridamole, Mebeverine Hydrochloride, Propylthiouracil, Quinidine Sulfate, and Topiramate Oral Suspensions in SyrSpend SF PH4 de Oliveira Ferreira Anderson, Polonini Hudson, Loures da Silva Sharlene, Buzinari Aglio Natália Cristina, Abreu Jordana, Fernandes Brandão Marcos Antônio Jul/Aug 2017 339-346 Buy
Transdermal Progesterone: Effects on Menopausal Symptoms and on Thrombotic, Anticoagulant, and Inflammatory Factors in Postmenopausal Women Stephenson Kenna, Neuenschwander Pierre F, Kurdowska Anna K, Pinson Barbara, Price Carol Jul/Aug 2008 295-304 Buy
The Effects of Compounded Bioidentical Transdermal Hormone Therapy on Hemostatic, Inflammatory, and Immune Factors; Cardiovascular Biomarkers; Quality of Life Measures; and Health Outcomes in Perimenopausal and Postmenopausal Women Stephenson Kenna, Neuenschwander Pierre F, Kurdowska Anna K Jan/Feb 2013 74-85 View Sample
The Science Behind Hormone Replacement Therapy, Part 1 Wepfer Scott T Nov/Dec 2001 462 Buy