Erbium:YAG fractional laser ablation improves cutaneous delivery of pentoxifylline from different topical dosage forms

• Published in: International journal of pharmaceutics Vol. 628; p. 122259
• Main Authors: Gou, Si, del Río-Sancho, Sergio, Laubach, Hans-Joachim, Kalia, Yogeshvar N.
• Format: Journal Article
• Language: English
• Published: Elsevier B.V 25.11.2022
• Subjects: Cutaneous delivery; Er:YAG fractional laser ablation; Pentoxifylline; Skin fibrosis; Topical dosage forms; Pentoxifylline; Topical dosage forms; Er:YAG fractional laser ablation; Cutaneous delivery; Skin fibrosis
• ISSN: 0378-5173; 1873-3476; 1873-3476
• DOI: 10.1016/j.ijpharm.2022.122259

[Display omitted] Topical application of pentoxifylline (PTX) would enable targeted treatment of radiation-induced skin fibrosis. However, PTX is hydrophilic with limited partitioning into the stratum corneum. The objective of this study was to investigate whether use of Erbium:YAG fractional laser ablation and different topical dosage forms (solution, hydrogel and patch) could be used to improve PTX cutaneous delivery as opposed to transdermal permeation. Initial results confirmed that fractional laser ablation significantly increased PTX delivery from each dosage form compared to passive controls. Delivery efficiencies of ∼ 30% were achieved with each dosage form but a large proportion of PTX permeated across the skin; thus, fluences were decreased to create shallower micropores, their depth being linearly dependent on fluence. The hydrogel was selected as the optimal formulation and PTX delivery efficiencies were further increased (44%-67%) by reducing the amount of hydrogel applied (better mimicking conditions of use). As this resulted in PTX depletion in the formulation, a loss of dependence of delivery on laser fluence was observed. These findings suggest that fractional laser ablation at moderate fluences enables an effective and targeted cutaneous delivery of PTX from a hydrogel formulation, which can be easily produced without the need for complex equipment.