Microneedle Patches Loaded with cRGD-Modified pH-Sensitive Hydroxycamptothecin Liposomes for Melanoma Therapy

Area of Science:

• Biomedical Engineering
• Nanotechnology
• Dermatology

Background:

• Melanoma treatment faces challenges like side effects and drug resistance.
• Chemotherapeutic transdermal delivery offers a promising strategy for melanoma therapy.
• Hydrophobic drugs require advanced delivery systems for effective treatment.

Purpose of the Study:

• To develop novel microneedle (MN) patches for transdermal delivery of 10-hydroxycamptothecin (HCPT) in melanoma.
• To create cRGD-modified pH-sensitive liposomes (cRGD-LP-HCPT) for targeted drug delivery and enhanced efficacy.
• To evaluate the therapeutic potential and safety of the cRGD-LP-HCPT MN patches for melanoma treatment.

Main Methods:

• Preparation of cRGD-modified pH-sensitive HCPT liposomes using thin-film hydration-ultrasonic method.
• Assembly of liposomes into water-soluble microneedle tips for transdermal drug delivery.
• Evaluation of liposome characteristics (size, encapsulation, release), cytotoxicity, microneedle properties, skin penetration, and in vivo tumor targeting.

Main Results:

• cRGD-LP-HCPT exhibited high encapsulation efficiency (94.78%), small size (∼102.91 nm), and pH-triggered release.
• The formulation showed enhanced cytotoxicity with an IC50 of 1 μg/mL compared to unmodified liposomes.
• Microneedle patches demonstrated good mechanical properties, successful skin penetration, and localized tumor targeting with minimal systemic exposure.

Conclusions:

• The developed cRGD-LP-HCPT MN patch is an effective system for transdermal melanoma therapy.
• This novel formulation enhances drug solubility, stability, targeting specificity, and intracellular accumulation.
• The cRGD-LP-HCPT MN patch shows significant antitumor efficiency and minimal side effects, indicating its clinical potential.