Nanosuspension-Loaded Dissolving Microneedle Patches for Enhanced Transdermal Delivery of a Highly Lipophilic Cannabidiol

• DOI: 10.2147/ijn.s452207
• Publication Date: 2024-05-07T04:55:13Z
• Authors: Aguo Cheng; Suohui Zhang; Fanda Meng; Mengzhen Xing; Han Liu; Guozhong Yang; Yunhua Gao
• Keywords: Male; Medicine (General); Microinjections; dissolving microneedle; Skin Absorption; Transdermal Patch; Administration, Cutaneous; Rats, Sprague-Dawley; cannabidiol; 03 medical and health sciences; R5-920; Drug Delivery Systems; Suspensions; Animals; Cannabidiol; Particle Size; nanosuspension; Original Research; Skin; 0303 health sciences; knee synovitis.; Rats; Solubility; Needles; Nanoparticles; highly lipophilic drugs

Purpose: Transdermal Drug Delivery System (TDDS) offers a promising alternative for delivering poorly soluble drugs, challenged by the stratum corneum's barrier effect, which restricts pool of drug candidates suitable TDDS. This study aims to establish delivery platform specifically highly lipophilic drugs requiring high doses (log P > 5, dose 10 mg/kg/d), improve their intradermal and enhance solubility. Methods: Cannabidiol (CBD, log = 5.91) served as model drug. A CBD nanosuspension (CBD-NS) was prepared using bottom-up method. The particle size, polydispersity index (PDI), zeta potential, concentration CBD-NS were characterized. Subsequently, incorporated into dissolving microneedles (DMNs) through one-step manufacturing process. dissolution abilities, physicochemical properties, mechanical strength, insertion depth, release behavior DMNs evaluated. Sprague-Dawley (SD) rats utilized assess efficacy DMN patch in treating knee synovitis analyze its skin permeation kinetics pharmacokinetic performance. Results: CBD-NS, stabilized with Tween 80, exhibited size 166.83 ± 3.33 nm, PDI 0.21 0.07, 46.11 0.52 mg/mL. loaded demonstrated favorable properties. It effectively increased skin, extended action's duration vivo, enhanced bioavailability. superior therapeutic safety rat synovitis, significantly inhibiting TNF-α IL-1β compared methotrexate subcutaneous injection Conclusion: NS technology enhances solubility CBD, while facilitates penetration, extends action improves Furthermore, has shown outcomes synovitis. innovative system is expected offer more efficient solution administration akin thereby facilitating high-dose administration. Keywords: nanosuspension, microneedle, cannabidiol,