The substantiation for the selection of excipients in the composition of the topical analgesic foam
DOI:
https://doi.org/10.24959/nphj.25.160Keywords:
dexpanthenol, lidocaine hydrochloride, topical anesthetic, excipients, propellant, topical foamAbstract
Skin aerosol foams are promising drug delivery systems due to their numerous advantages and ease of use. The application of foam minimizes the need for touching and rubbing the damaged skin, as the foam spreads easily on the skin with minimal to moderate shear force, which is particularly beneficial for treating wounds of various etiologies. Numerous scientific studies have demonstrated that the pharmaceutical combination of dexpanthenol and lidocaine creates an effective formulation for treating skin conditions due to their anti-inflammatory, antipruritic, anesthetic, and antiseptic properties.
The aim of the study was to justify the selection of excipients in the composition of topical analgesic foam to ensure its stability, effectiveness, ease of application, and therapeutic properties.
Results and Discussion
The composition of a topical analgesic foam containing dexpanthenol at a concentration of 50 mg/ml and lidocaine hydrochloride at 15 mg/ml was developed and justified. A technological process for manufacturing the foam was proposed.
The use of excipients, including solvents, plasticizers, foam boosters, and foam stability stabilizers, was characterized, ensuring the formation of stable foam. The compatibility of aerosol solution components with the propellant was studied under various storage temperatures (2–8°C, 25°C, 37°C). The results confirm that the developed foam composition meets pharmacopoeial requirements for stability, efficacy, and consumer properties. This allows recommending the developed formulation for further research and practical application.
Conclusions
Optimal concentrations of excipients and propellant were justified to ensure appropriate consumer properties. It was determined that a propane-butane content in the range of 33.25–35.0 g provides optimal foam delivery characteristics, including stability (up to 40 minutes) and a high release percentage (over 93%). The pH of the primary solution (5.1–5.5) corresponds to the optimal range for the skin (4–6.5), ensuring patient comfort, minimizing irritation, and promoting wound healing processes. Further studies are aimed at the biopharmaceutical evaluation of the dosage form.
References
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Parsa M., Trybala A., Malik D.J., Starov V. (2019). Foam in pharmaceutical and medical applications. Curr Opin Colloid Interface Sci.;44:153–67. doi:10.1016/j.cocis.2019.10.007.
Arzhavitina A., Steckel H. (2010). Foams for pharmaceutical and cosmetic application. International Journal of Pharmaceutics.;394(1–2):1–17. doi:10.1016/j.ijpharm.2010.04.028.
Cho Y.S., Kim H.O., Woo S.M., Lee D.H. (2022). Use of Dexpanthenol for Atopic Dermatitis-Benefits and Recommendations Based on Current Evidence. Journal of Clinical Medicine;11(14):3943. doi:10.3390/jcm11143943.
Peng L., Zheng H.Y., Dai Y. (2019). Local dermal application of a compound lidocaine cream in pain management of cancer wounds. Brazilian Journal of Medical and Biological Research.;52(11):e8567. doi:10.1590/1414-431X20198567. PMID: 31721905; PMCID: PMC6853073.
Сompendium online [Internet]. Available from: http://compendium.com.ua.
Sezgin Y., Bilgin Çetin M., Bulut Ş., Alptekin N.Ö., Börçek P. (2019). Evaluating the Effects of a Topical Preparation with Dexpanthenol, Silbiol, Undecylenic Acid, and Lidocaine on Palatal Mucosa Wound Healing in a Rat Model. Balkan Medical Journal.;36(2):88–95. doi:10.4274/balkanmedj.galenos.2018.2018.0167. PMID: 30322831.
Palchevska T.A., Saliy O.O., Baula O.P., Palchevskyi K.V., Onishchuk O.M. (2021). The role of excipients of trometamolum and meglumine in the formation of biopharmaceutical properties of medicinal products of various pharmacites. Farmatsevtychnyi Zhurnal, 76, 4, 64-75. doi:10.32352/0367-3057.4.21.06.
Gennari C.G.M., Selmin F., Minghetti P., Cilurzo F. (2019). Medicated Foams and Film Forming Dosage Forms as Tools to Improve the Thermodynamic Activity of Drugs to be Administered Through the Skin. Current Drug Delivery.;16(5):461–71. doi:10.2174/1567201816666190118124439. PMID: 30657040;
USP <601>. Aerosols, Nasal Sprays, Metered-Dose Inhalers, and Dry Powder Inhalers [Internet]. Available from: http://www.uspbpep.com/usp31/v31261/usp31nf26s1_c601.asp#google_vignette.
Moreno Y.S., Bournival G., Ata S. (2021). Foam stability of flotation frothers under dynamic and static conditions. Separation and Purification Technology.;274:117822. https://doi.org/10.1016/j.seppur.2020.117822
Seweryn A. (2018). Interactions between surfactants and the skin - Theory and practice. Advances in Colloid and Interface Science ;256:242–55. doi:10.1016/j.cis.2018.04.002. PMID: 29685575.
Chang Q. (2016). Emulsion, foam, and gel. In: Colloid and Interface Chemistry for Water Quality Control. Cambridge: Academic Press;. p. 227–45.
Fameau A.L., Ventureira J., Novales B., Douliez J.P. (2012). Foaming and emulsifying properties of fatty acids neutralized by tetrabutylammonium hydroxide. Colloids and Surfaces A: Physicochemical and Engineering Aspects.;403:87–95. doi:10.1016/j.colsurfa.2012.03.059.
Garner N., Siol A., Eilks I. (2014). Parabens as preservatives in personal care products. Chem Action.;(103):36–43.
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