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Risperidone-cyclodextrin complex reservoir combined with hydrogel-forming microneedle array patches for enhanced transdermal delivery.
Ghanma, Rand; Anjani, Qonita Kurnia; Naser, Yara A; Sabri, Akmal Hidayat Bin; Hutton, Aaron R J; Vora, Lalitkumar K; Himawan, Achmad; Greer, Brett; McCarthy, Helen O; Donnelly, Ryan F.
Affiliation
  • Ghanma R; School of Pharmacy, Queen's University Belfast, Medical Biology Centre, 97 Lisburn Road, Belfast BT9 7BL, UK; Department of Pharmaceutical Technology, Faculty of Pharmacy, Jordan University of Science and Technology, Irbid, Jordan.
  • Anjani QK; School of Pharmacy, Queen's University Belfast, Medical Biology Centre, 97 Lisburn Road, Belfast BT9 7BL, UK.
  • Naser YA; School of Pharmacy, Queen's University Belfast, Medical Biology Centre, 97 Lisburn Road, Belfast BT9 7BL, UK.
  • Sabri AHB; School of Pharmacy, Queen's University Belfast, Medical Biology Centre, 97 Lisburn Road, Belfast BT9 7BL, UK.
  • Hutton ARJ; School of Pharmacy, Queen's University Belfast, Medical Biology Centre, 97 Lisburn Road, Belfast BT9 7BL, UK.
  • Vora LK; School of Pharmacy, Queen's University Belfast, Medical Biology Centre, 97 Lisburn Road, Belfast BT9 7BL, UK.
  • Himawan A; School of Pharmacy, Queen's University Belfast, Medical Biology Centre, 97 Lisburn Road, Belfast BT9 7BL, UK.
  • Greer B; Institute for Global Food Security, School of Biological Science, Queen's University Belfast, 19 Chlorine Gardens, Belfast BT9 5DL, UK.
  • McCarthy HO; School of Pharmacy, Queen's University Belfast, Medical Biology Centre, 97 Lisburn Road, Belfast BT9 7BL, UK.
  • Donnelly RF; School of Pharmacy, Queen's University Belfast, Medical Biology Centre, 97 Lisburn Road, Belfast BT9 7BL, UK. Electronic address: r.donnelly@qub.ac.uk.
Eur J Pharm Biopharm ; 202: 114415, 2024 Sep.
Article in En | MEDLINE | ID: mdl-39013492
ABSTRACT
Hydrogel-forming microneedle array patches (HFMAPs) are microneedles that create microconduits upon insertion and swelling in the skin, potentially allowing prolonged drug delivery without generating sharps waste. Delivering hydrophobic drugs using HFMAPs poses challenges, which can be addressed using solubility enhancers such as cyclodextrins (CDs). This study aimed to deliver risperidone (RIS) transdermally using HFMAPs. To enhance the aqueous solubility of RIS hydroxypropyl-beta-cyclodextrin (HP-ß-CD) and hydroxypropyl-gamma-cyclodextrin (HP-γ-CD) were utilised and their performance was tested using phase solubility studies. The aqueous solubility of RIS was enhanced by 4.75-fold and 2-fold using HP-ß-CD and HP-γ-CD, respectively. RIS-HP-ß-CD complex (CX) and physical mixture (PM) directly compressed tablets were prepared and combined with HFMAPs. Among the tested formulations, RIS-HP-ß-CD PM reservoirs with 11 x 11 PVA/PVP HFMAPs exhibited the best performance in ex vivo studies and were further evaluated in in vivo experiments using female Sprague Dawley rats. The extended wear time of the MAPs resulted in the sustained release of RIS and its active metabolite 9-hydroxyrisperidone (9-OH-RIS) in plasma samples, lasting from 3 to 5 days with a 1-day application and up to 10 days with a 5-day application. For a 1-day application, HFMAPs showed greater systemic exposure to RIS compared to intramuscular control (AUC0-t 13330.05 ± 2759.95 ng/mL/hour versus 2706 ± 1472 ng/mL/hour). Moreover, RIS exposure was extended to 5 days (AUC0-t 12292.37 ± 1801.94 ng/mL/hour). In conclusion, HFMAPs could serve as an alternative for delivering RIS in a sustained manner, potentially improving the treatment of schizophrenia.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Solubility / Administration, Cutaneous / Drug Delivery Systems / Risperidone / Hydrogels / 2-Hydroxypropyl-beta-cyclodextrin Limits: Animals Language: En Journal: Eur J Pharm Biopharm Journal subject: FARMACIA / FARMACOLOGIA Year: 2024 Document type: Article Affiliation country: Jordan Country of publication: Netherlands

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Solubility / Administration, Cutaneous / Drug Delivery Systems / Risperidone / Hydrogels / 2-Hydroxypropyl-beta-cyclodextrin Limits: Animals Language: En Journal: Eur J Pharm Biopharm Journal subject: FARMACIA / FARMACOLOGIA Year: 2024 Document type: Article Affiliation country: Jordan Country of publication: Netherlands