Fabrication, characterization and comparison of α-arbutin loaded dissolving and hydrogel forming microneedles

• Published in: International journal of pharmaceutics Vol. 586; p. 119508
• Main Authors: Aung, Nway Nway, Ngawhirunpat, Tanasait, Rojanarata, Theerasak, Patrojanasophon, Prasopchai, Pamornpathomkul, Boonnada, Opanasopit, Praneet
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 30.08.2020
• Subjects: Administration, Cutaneous; Animals; Arbutin - administration & dosage; Arbutin - chemistry; Arbutin - pharmacokinetics; Dissolving microneedles; Drug Carriers - chemistry; Drug Delivery Systems; Drug Stability; Drug Storage; Hydrogel forming microneedles; Hydrogels; Hydrophobic and Hydrophilic Interactions; Permeability; Polymethacrylic Acids - chemistry; Polyvinyl Alcohol - chemistry; Skin - metabolism; Skin Absorption; Skin lightening; Skin Lightening Preparations - administration & dosage; Skin Lightening Preparations - chemistry; Skin Lightening Preparations - pharmacokinetics; Swine; Transdermal; α-Arbutin; Dissolving microneedles; Transdermal; α-Arbutin; Skin lightening; Hydrogel forming microneedles
• DOI: 10.1016/j.ijpharm.2020.119508
• ISSN: 0378-5173

[Display omitted] In this study, polyacrylic acid-co-maleic acid (PAMA) and polyvinyl alcohol (PVA) (1:4) were used to fabricate dissolving microneedles (DMNs) and hydrogel forming microneedles (HMNs) which incorporated α-arbutin. Αlpha-arbutin is commonly used as a skin lightening agent. However, it has poor penetration ability due to its hydrophilic properties. The purpose of this study was to compare the permeation of α-arbutin into the skin using DMNs and HMNs. Both types of microneedles (MNs) were sharp, strong with elegant appearance and approximately 100% penetrated the neonatal porcine skin. All needles of α-arbutin loaded DMNs were completely dissolved within 45 min, whereas maximum swelling of HMNs was observed at 4 h. In vitro permeation studies showed that α-arbutin loaded DMNs and HMNs provided significantly about 4.5 and 2.8 times, respectively, greater α-arbutin permeability than gel and commercial cream (P < 0.05). In vivo study also showed high intradermal delivery of α-arbutin levels using DMNs (5.33 µg/mL) and HMNs (1.47 µg/mL) when compared to that of commercial cream 0.15 µg/mL. Moreover, the micro-holes caused by applying MNs can reseal within 1 h. MNs were also stable at 25 °C for 3 months. The results suggested that DMNs and HMNs developed have a promising platform for transdermal delivery.