TY - JOUR
T1 - Combination of Dissolving Microneedles with Nanosuspension and Co-Grinding for Transdermal Delivery of Ketoprofen
AU - Ramadon, Delly
AU - Ulayya, Fathin
AU - Qur’ani, Annisa Sakinah
AU - Iskandarsyah, Iskandarsyah
AU - Harahap, Yahdiana
AU - Anjani, Qonita Kurnia
AU - Aileen, Vania
AU - Hartrianti, Pietradewi
AU - Donnelly, Ryan F.
N1 - Funding Information:
The authors thank the Ministry of Education, Culture, Research, and Technology who has supported this research (Hibah Penelitian Dasar Kompetitif Nasional 2022; NKB-883/UN2.RST/HKP.05.00/2022). The authors also thank the School of Pharmacy, Queen’s University Belfast (Northern Ireland, The United Kingdom) and the School of Life Sciences, Indonesia International Institute for Life-Sciences (Jakarta, Indonesia), for sharing their facilities and instruments used in this research.
Funding Information:
This research was funded by the Ministry of Education, Culture, Research, and Technology (Hibah Penelitian Dasar Kompetitif Nasional 2022; NKB-883/UN2.RST/HKP.05.00/2022).
Publisher Copyright:
© 2023 by the authors.
PY - 2023/3
Y1 - 2023/3
N2 - Ketoprofen is an anti-inflammatory agent that may cause gastric irritation if administered orally. Dissolving microneedles (DMN) can be a promising strategy to overcome this issue. However, ketoprofen has a low solubility; therefore, it is essential to enhance its solubility using certain methods, namely nanosuspension (NS) and co-grinding (CG). This research aimed to formulate DMN containing ketoprofen-loaded NS and CG. Ketoprofen NS was formulated with poly(vinyl alcohol) (PVA) at concentrations of 0.5%, 1%, and 2%. CG was prepared by grinding ketoprofen with PVA or poly(vinyl pyrrolidone) (PVP) at different drug–polymer ratios. The manufactured ketoprofen-loaded NS and CG were evaluated in terms of their dissolution profile. The most promising formulation from each system was then formulated into microneedles (MNs). The fabricated MNs were assessed in terms of their physical and chemical properties. An in vitro permeation study using Franz diffusion cells was also carried out. The most promising MN-NS and MN-CG formulations were F4-MN-NS (PVA 5%-PVP 10%), F5-MN-NS (PVA 5%-PVP 15%), F8-MN-CG (PVA 5%-PVP 15%), and F11-MN-CG (PVA 7.5%-PVP 15%), respectively. The cumulative amounts of drug permeated after 24 h for F5-MN-NS and F11-MN-CG were 3.88 ± 0.46 µg and 8.73 ± 1.40 µg, respectively. In conclusion, the combination of DMN with nanosuspension or a co-grinding system may be a promising strategy for delivering ketoprofen transdermally.
AB - Ketoprofen is an anti-inflammatory agent that may cause gastric irritation if administered orally. Dissolving microneedles (DMN) can be a promising strategy to overcome this issue. However, ketoprofen has a low solubility; therefore, it is essential to enhance its solubility using certain methods, namely nanosuspension (NS) and co-grinding (CG). This research aimed to formulate DMN containing ketoprofen-loaded NS and CG. Ketoprofen NS was formulated with poly(vinyl alcohol) (PVA) at concentrations of 0.5%, 1%, and 2%. CG was prepared by grinding ketoprofen with PVA or poly(vinyl pyrrolidone) (PVP) at different drug–polymer ratios. The manufactured ketoprofen-loaded NS and CG were evaluated in terms of their dissolution profile. The most promising formulation from each system was then formulated into microneedles (MNs). The fabricated MNs were assessed in terms of their physical and chemical properties. An in vitro permeation study using Franz diffusion cells was also carried out. The most promising MN-NS and MN-CG formulations were F4-MN-NS (PVA 5%-PVP 10%), F5-MN-NS (PVA 5%-PVP 15%), F8-MN-CG (PVA 5%-PVP 15%), and F11-MN-CG (PVA 7.5%-PVP 15%), respectively. The cumulative amounts of drug permeated after 24 h for F5-MN-NS and F11-MN-CG were 3.88 ± 0.46 µg and 8.73 ± 1.40 µg, respectively. In conclusion, the combination of DMN with nanosuspension or a co-grinding system may be a promising strategy for delivering ketoprofen transdermally.
KW - co-grinding
KW - dissolving microneedles
KW - ketoprofen
KW - nanosuspension
KW - solubility
UR - http://www.scopus.com/inward/record.url?scp=85151742905&partnerID=8YFLogxK
U2 - 10.3390/ph16030378
DO - 10.3390/ph16030378
M3 - Article
AN - SCOPUS:85151742905
SN - 1424-8247
VL - 16
JO - Pharmaceuticals
JF - Pharmaceuticals
IS - 3
M1 - 378
ER -