Delivery of Poorly Water Soluble Lidocaine by Dissolving Microneedles / 中国药学杂志

ABSTRACT

OBJECTIVE: To prepare dissolving microneedles using Gantrez S-97 and PVPk30 as composite matrix materials to accelerate the delivery of poorly water soluble drugs and study the preparation, appearance, mechanical properties, intradermal solubility, drug efficacy and crystallization behavior of dissolving microneedles. METHODS: Using polydimethylsiloxane(PDMS) as the negative mode, microneedles were prepared by the reverse casting method. SEM was used to observe the morphological appearance of the microneedles. The mechanical properties of the microneedles were investigated by texture analyzer and histological sections. Delivery of lidocaine was characterized by intradermal dissolution and pharmacodynamics. Crystallization behavior of lidocaine was characterized by DSC. RESULTS: Lidocaine dissolving microneedles had good needle shape and possessed sufficient mechanical strength to penetrate into the skin. The microneedles could dissolve in the dermis within 3 min and retain anesthetic effect, and the drug existed in amorphous form in the microneedles. CONCLUSION: Cosolvent preparation of dissolving microneedles has potential for promoting the delivery of poorly water soluble drugs.