Compatibility studies of lapachol with pharmaceutical excipients for the development of topical formulations

Compatibility studies of lapachol with pharmaceutical excipients for the development of topical formulations

Among naphthoquinones, lapachol and many heterocyclic derivatives have been investigated during the past years, mainly due to their antibacterial, antifungal and anticancer activities. Assessment of possible incompatibility between an active component (i.e. lapachol) and different excipients along w...

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Bibliographic Details
Published in:Thermochimica acta Vol. 457; no. 1; pp. 1 - 6
Main Authors: Lira, A.M., Araújo, A.A.S., Basílio, I.D.J., Santos, B.L.L., Santana, D.P., Macedo, R.O.
Format: Journal Article
Language:English
Published: Amsterdam Elsevier B.V 15-06-2007
Elsevier Science
Subjects:
Analysis
Biological and medical sciences
Compatibility studies
DSC
Gel-cream
General pharmacology
Lapachol
Medical sciences
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Compatibility studies
Lapachol
DSC
Gel-cream
Antineoplastic agent
Antimalarial
Differential scanning calorimetry
Cream
Vehicle(excipient)
Naphthoquinone derivatives
Naphthalene derivatives
Percutaneous route
Formulation
Dosage form
Parasiticide
Thermal analysis
Compatibility
Topical administration
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Summary:Among naphthoquinones, lapachol and many heterocyclic derivatives have been investigated during the past years, mainly due to their antibacterial, antifungal and anticancer activities. Assessment of possible incompatibility between an active component (i.e. lapachol) and different excipients along with the evaluation of thermal stability are crucial parts of a normal study prior to the final formulation setting of a medicine. DSC study was used as an important and complementary tool during pre-formulation to determine the compatibility of drug-excipients with the purpose of developing a lapachol gel-cream formulation. The DSC curves of lapachol (Lpch) and binary mixtures with excipients (propylparaben, methylparaben, edetic acid, isodecyl oleate, trietanolamine, glyceril monoesterate, cetiol, glicerin, carbopol, cetomacrogol and mineral oil) were obtained. The results showed that Lpch only exhibited interaction which could influence the stability of the product in the binary mixtures of Lpch/methylparaben, Lpch/cetostearyl alcohol and Lpch/glyceryl monostearate. There was a significant shift or absence of lapachol melting peak in both cases. Photovisual DSC was used to confirm the results obtained with conventional DSC because it is a more sensitive method.
ISSN:0040-6031
1872-762X
DOI:10.1016/j.tca.2007.02.017