New Skin Treatment Boosts Local Anesthetic Absorption

Authors
Journal
Pharmaceutical Research
Year
DOI
10.1007/s11095-026-04064-w
Study Type
Guinea Pig
Outcome
Positive
Peer Reviewed
Yes
Country
China
Health Condition
Skin Conditions
Body System
Integumentary

TL;DR

Calcium hydrogen phosphate particles improved transdermal drug delivery by gently disrupting the stratum corneum, increasing skin permeation and shortening the onset time of topical lidocaine-tetracaine anesthesia in guinea pigs.

Summary

This formulation study evaluated whether calcium hydrogen phosphate particles could be used as mild dermabrasion agents to improve transdermal drug delivery. Gentle rubbing of the particles on skin disrupted the stratum corneum barrier and increased permeation of fluorescent model compounds, including FITC and FITC-Dextran4000, as well as a lidocaine-tetracaine eutectic microemulsion gel. The permeation effect increased with larger particle size, higher particle amount, greater rubbing pressure, and longer rubbing duration. In guinea pigs, the calcium hydrogen phosphate-containing anesthetic gel shortened onset time and improved local anesthetic efficacy in a needle-prick model. These findings suggest that calcium hydrogen phosphate particles may offer a tolerable mechanical strategy for enhancing skin penetration of topical bioactive compounds.

Abstract (excerpt)

Background: Transdermal drug delivery (TDD) offers a convenient administration for treating local or systemic diseases. However, the dense "brick-mortar" structure of the stratum corneum hinders the skin permeation of most of bioactive molecules, which highly constrained the application of TDD…

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