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Systemic delivery of artemether by dissolving microneedles
Yuqin Qiu1, Chun Li1, Suohui Zhang1
1Key Laboratory of Photochemical Conversion and Optoelectronic Materials, Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Beijing, 100190, China.
International Journal of Pharmaceutics
|May 7, 2016
Summary
Dissolving microneedles effectively deliver poorly water-soluble drugs like artemether (ARM) transdermally. This minimally invasive approach shows comparable bioavailability and therapeutic effects to injections, offering a promising alternative for systemic drug delivery.
Area of Science:
- Pharmaceutical Sciences
- Biomaterials Engineering
- Drug Delivery Systems
Background:
- Transdermal drug delivery using dissolving microneedles (DMNs) offers a minimally invasive alternative to traditional methods.
- Systemic delivery of poorly water-soluble drugs via DMNs remains a significant challenge.
- Artemether (ARM), a poorly water-soluble antimalarial drug, serves as a model for developing advanced drug delivery systems.
Purpose of the Study:
- To develop and evaluate artemether (ARM)-loaded dissolving microneedles (DMNs) for efficient transdermal delivery.
- To assess the skin penetration, systemic absorption, and pharmacokinetic profile of ARM delivered via DMNs.
- To investigate the therapeutic efficacy of ARM-loaded DMNs in a relevant preclinical model.
Main Methods:
- Fabrication of ARM-loaded DMNs and characterization of their drug loading and release properties.
- Confocal laser scanning microscopy (CLSM) to visualize skin micro-conduits and determine needle insertion depth.
- In vivo pharmacokinetic studies in rats and pharmacodynamic evaluation in collagen-induced arthritis (CIA) rat models.
Main Results:
- DMNs successfully created micro-conduits in the skin, with an insertion depth of approximately 270μm.
- Maximum skin delivery of ARM reached 72.67±2.69% of the initial dose.
- Pharmacokinetic studies revealed a dose-dependent profile, with DMNs achieving comparable bioavailability and AUC to intramuscular injection, but with sustained plasma concentrations at 8h.
- Pharmacodynamic studies demonstrated that ARM-loaded DMNs effectively reversed paw edema in CIA rats, similar to intramuscular ARM.
Conclusions:
- Developed ARM-loaded DMNs provide an effective and minimally invasive strategy for the systemic delivery of poorly water-soluble drugs.
- This transdermal approach offers comparable therapeutic outcomes to traditional intramuscular injections.
- DMNs represent a promising platform for improving drug delivery and patient compliance for challenging drug molecules.
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