Topical Treatment of Infantile Haemangiomas: A Comparative Study on the Selection of a Semi-Solid Vehicle

Abstract

Background/Aim: Topical β-blockers have recently been proposed as a valid alternative to oral drugs for treating cutaneous infantile haemangiomas, but clinical results in the literature are inconsistent due to the empirical choice of topical preparations. The current investigation aimed to rationalize the selection of a semi-solid vehicle for a locally applied drug product containing 1% w/w propranolol hydrochloride (PR-Cl). Methods: A hydrophobic ointment of PR-Cl, two lipophilic creams, and a hydrophilic cream were prepared. In vitro release and skin permeation studies through human epidermis and full-thickness skin were performed by Franz diffusion cells. Results: The overall results highlighted that PR-Cl was able to permeate the human epidermis, and its penetration pattern was strongly influenced by the composition of the semi-solid vehicle. PR-Cl release and permeation from lipophilic vehicles were extremely limited and influenced by their composition. Best results were obtained by using the hydrophilic cream. Furthermore, the retention study evidenced that epidermis acted as a reservoir, releasing the PR-Cl accumulated after preparation removal. Conclusion: The 1% w/w PR-Cl cream resulted the most suitable formulation for improving drug permeation through the human epidermis. On the contrary, the negligible permeation profile through full-thickness skin pointed out that PR-Cl cannot diffuse significantly to reach the deeper layers of human skin.

Emulsion versus nanoemulsion: how much is the formulative shift critical for a cosmetic product?

“…Considering the lower water concentration of this formulation with respect to the nanoemulsion (i.e. 30 vs 70%), such enhancement effect may be caused by the higher thermodynamic activity of CAF inside the gel-like structure [21]; higher occlusive properties could also influence this result [22]. The closeness to maximum solubility of CAF is evidenced by preliminary stability studies.…”

Development and Characterization of Nanoemulsion Containing Almond Oil, Biodegradable Polymer and Propranolol as Potential Treatment in Hemangioma

“…Many studies have shown the efficacy and safety of topical use of POP in the treatment of superficial IHs . It was observed that the treatment with 1% w/w of POP cream and 1% w/w of propranolol hydrophilic ointment were well tolerated without side effects, which indicates that the topical application is a safe, effective and cheap therapeutic option for treating superficial IHs .…”

“…Indeed, the amount of drug retained in the human epidermis (54.57 μg cm −2 ) can diffuse to the superficial hemangioma maintaining a clinical effect. In particular, lipophilic creams may also take advantage of the occlusive effect and be able to sustain drug penetration in the human epidermis …”

“…[1,4,5,8] It was observed that the treatment with 1% w/w of POP cream and 1% w/w of propranolol hydrophilic ointment were well tolerated without side effects, which indicates that the topical application is a safe, effective and cheap therapeutic option for treating superficial IHs. [2] Moreover, Casiraghi et al (2016) selected a semi-solid vehicle (e.g. hydrophilic ointment, two lipophilic creams and hydrophilic cream) for a locally applied drug product containing 1% w/w of propranolol hydrochloride and studied the skin permeation through human epidermis.…”

“…In particular, lipophilic creams may also take advantage of the occlusive effect and be able to sustain drug penetration in the human epidermis. [8] An ideal drug delivery system fulfills the objective of maximizing therapeutic effect while minimizing toxicity. [9] Nanoemulsion (NE) is a drug delivery system constituted by nanodroplets with a size between 20 and 200 nm surrounded by surfactant.…”