EVALUASI SISTEM PENGHANTARAN OBAT TRANSDERMAL BERBASIS MICRONEEDLE: TINJAUAN KARAKTERISASI, FARMAKOKINETIK, EFIKASI, STABILITAS, DAN KEAMANAN

KIKI KANIA, - (2026) EVALUASI SISTEM PENGHANTARAN OBAT TRANSDERMAL BERBASIS MICRONEEDLE: TINJAUAN KARAKTERISASI, FARMAKOKINETIK, EFIKASI, STABILITAS, DAN KEAMANAN. Health Research Journal of Indonesia (HRJI), 4 (5). pp. 1987-2004. ISSN 2964-7592

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Abstract

Pendahuluan: Microneedle merupakan sistem penghantaran obat transdermal inovatif yang menggunakan jarum berukuran mikro (150–1500 μm) untuk menembus stratum corneum secara minimal invasif. Meskipun teknologi ini telah berkembang sejak akhir 1990-an, panduan terintegrasi mengenai parameter evaluasi yang harus dilakukan dalam pengembangan microneedle masih terbatas, sehingga menyulitkan standardisasi metode dan komparasi hasil antar studi. Tujuan: Review ini bertujuan menyusun kerangka sistematis parameter evaluasi yang perlu dilakukan dalam karakterisasi dan pengembangan sediaan microneedle, yang mencakup enam domain utama: karakterisasi struktur dan sifat fisik, evaluasi sediaan, profil farmakokinetik, efikasi, stabilitas, dan keamanan. Metode: Penelusuran literatur secara naratif-sistematis dilakukan pada basis data PubMed, ScienceDirect, dan Google Scholar terhadap publikasi periode 2018–2025 menggunakan kata kunci microneedleyang dikombinasikan dengan operator Boolean AND/OR. Kriteria inklusi meliputi artikel penelitian asli berbahasa Inggris pada microneedle berbasis polimer yang dimuat zat aktif dan melaporkan minimal satu parameter evaluasi. Hasil: Identifikasi literatur menghasilkan enam domain evaluasi yang harus dilakukan: (1) karakterisasi struktur melalui Scanning Electron Microscopy (SEM), pengukuran kekuatan mekanik (rentang 0,22–32 N), dan ketebalan patch (38 μm–1 mm); (2) evaluasi sediaan melalui insertion test (kedalaman penetrasi 200–600 μm), drug loading (38–99%), uji disolusi (1,5–20 menit), uji difusi Franz cell, dan kadar kelembapan (2,25–3,8%); (3) studi farmakokinetik in vivo yang ditunjukkan pada patch microneedle cannabidiol dengan bioavailabilitas relatif 144,70% dibandingkan injeksi subkutan; (4) evaluasi efikasi yang disesuaikan dengan indikasi terapeutik (antikanker, antidiabetes, antiinflamasi, antihipertensi, antibakterial, dan dermatologi); (5) uji stabilitas mengacu pada pedoman ICH Q1A (R2) dengan kondisi dipercepat, intermediet, dan jangka panjang; serta (6) evaluasi keamanan melalui uji iritasi Draize dengan parameter Primary Irritation Index (PII) yang menunjukkan iritasi ringan dan reversibel. Simpulan: Pengembangan sediaan microneedle yang berkualitas mensyaratkan pelaksanaan keenam domain evaluasi secara terpadu. Kerangka sistematis ini dapat menjadi acuan standar bagi peneliti dan pengembang microneedle di Indonesia, sekaligus mendorong harmonisasi metode evaluasi dengan pedoman internasional untuk memfasilitasi translasi klinis dan registrasi produk domestik. ------- Introduction: Microneedles are innovative transdermal drug delivery systems that employ micro-sized needles (150–1500 μm) to penetrate the stratum corneum in a minimally invasive manner. Although this technology has been developed since the late 1990s, an integrated reference outlining the evaluation parameters required in microneedle development remains limited, hindering method standardization and inter-study comparison. Objective: This review aims to construct a systematic framework of evaluation parameters that must be performed in the characterization and development of microneedle preparations, encompassing six main domains: structural and physical characterization, formulation evaluation, pharmacokinetic profile, efficacy, stability, and safety. Methods: A narrative-systematic literature search was conducted in PubMed, ScienceDirect, and Google Scholar for publications between 2018 and 2025 using microneedle-related keywords combined with Boolean AND/OR operators. Inclusion criteria comprised original research articles in English on polymer-based microneedles loaded with active substances that reported at least one evaluation parameter. Results: Six required evaluation domains were identified: (1) structural characterization through Scanning Electron Microscopy (SEM), mechanical strength measurement (range 0.22–32 N), and patch thickness (38 μm–1 mm); (2) formulation evaluation through insertion test (penetration depth 200–600 μm), drug loading (38–99%), dissolution test (1.5–20 min), Franz cell diffusion, and moisture content (2.25–3.8%); (3) in vivo pharmacokinetic studies, exemplified by the cannabidiol microneedle patch showing 144.70% relativebioavailability compared to subcutaneous injection; (4) efficacy evaluation tailored to therapeutic indications (anticancer, antidiabetic, anti-inflammatory, antihypertensive, antibacterial, and dermatologic); (5) stability testing under ICH Q1A (R2) guidelines at accelerated, intermediate, and long-term conditions; and (6) safety evaluation via the Draize irritation test using the Primary Irritation Index (PII), which demonstrated mild and reversible irritation. Conclusion: Quality development of microneedle preparations requires integrated execution of all six evaluation domains. This systematic framework can serve as a standard reference for microneedle researchers and developers in Indonesiawhile promoting harmonization of evaluation methods with international guidelines to facilitate clinical translation and domestic product registration.

Item Type:	Article
Uncontrolled Keywords:	microneedle, transdermal, karakterisasi, farmakokinetik, evaluasi keamanan. ----- microneedle, transdermal, characterization, pharmacokinetics, safety evaluation
Subjects:	R Medicine > R Medicine (General) R Medicine > RM Therapeutics. Pharmacology
Divisions:	Program Studi Magister Farmasi > Publikasi Artikel Ilmiah
Depositing User:	pustakawan - -
Date Deposited:	02 Nov 2026 02:58
Last Modified:	02 Nov 2026 02:59
URI:	http://repository.stfi.ac.id/id/eprint/4899

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