Enhancement of skin localization of β-carotene from red fruit (Pandanus conoideus Lam.) using solid dispersion-thermoresponsive gel delivered via polymeric solid microneedles

[Display omitted] •Beta carotene extract from Papuan red fruit were incorporated into solid dispersion.•Solid dispersion-loaded thermoresponsive gel delivered by polymeric solid microneedles.•The combination showed desirable characteristics for enhanced skin localization.•In vitro release exhibits a...

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Veröffentlicht in:International journal of pharmaceutics 2024-07, Vol.660, p.124307, Article 124307
Hauptverfasser: Fitri, Andi Maqhfirah Nurul, Mahfufah, Ulfah, Aziz, Sumayya Binti Abd, Sultan, Nurul Aisha Fitri, Mahfud, Muhammad Alif Sya’ban, Saputra, Mesakh Diki, Elim, Diany, Bakri, Nur Fadillah, Arjuna, Andi, Sari, Yessie Widya, Domínguez-Robles, Juan, Pamornpathomkul, Boonnada, Mir, Maria, Permana, Andi Dian
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Sprache:eng
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Zusammenfassung:[Display omitted] •Beta carotene extract from Papuan red fruit were incorporated into solid dispersion.•Solid dispersion-loaded thermoresponsive gel delivered by polymeric solid microneedles.•The combination showed desirable characteristics for enhanced skin localization.•In vitro release exhibits a seven-fold increase compared to plain hydrogel.•The combination enhanced in vivo dermato-pharmakokinetic parameters by 200–400%. Red fruit (Pandanus conoideus Lam.) boasts high β-carotene (BC) content, often consumed orally. However, absorption issues and low bioavailability due to food matrix interaction have led to transdermal delivery exploration. Nevertheless, BC has a short skin retention time. To address these limitations, this study formulates a β-carotene solid dispersion (SD-BC) loaded thermoresponsive gel combined with polymeric solid microneedles (PSM) to enhance in vivo skin bioavailability. Characterization of SD-BC includes saturation solubility, X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (FTIR), and in vitro release. Characterization of SD-BC thermoresponsive gel includes gelation temperature, viscosity, rheological behaviour, pH, bio-adhesiveness, spreadability, and extrudability. PSM’s mechanical properties and insertion capability were assessed. Ex vivo and in vivo dermato-pharmacokinetic studies, drug content, hemolysis, and skin irritation assessments were conducted to evaluate overall performance. Results confirm amorphous SD-BC formation, enhancing solubility. Both SD-BC thermoresponsive gel and PSM exhibit favourable characteristics, including rheological properties and mechanical strength. In vitro release studies showed a seven-fold increase in BC release compared to plain hydrogel. SD-BC thermoresponsive gel combined with PSM achieves superior ex vivo permeation (Cmax = 305.43 ± 32.07 µg.mL−1) and enhances in vivo dermato-pharmacokinetic parameters by 200–400 %. Drug content, hemolysis, and skin irritation studies confirmed its safety and non-toxicity.
ISSN:0378-5173
1873-3476
1873-3476
DOI:10.1016/j.ijpharm.2024.124307