A1 Vertaisarvioitu alkuperäisartikkeli tieteellisessä lehdessä
Formulation and evaluation of poly(jasmine lactone) based micelles for improving the oral permeability of acyclovir
Tekijät: Verma, Jyoti; Frejborg, Fanny; Mantegna, Marta; Kumar, Vishal; Hukkanen, Veijo; Flaten, Gøril Eide; Rosenholm, Jessica M.; Bansal, Kuldeep K.
Kustantaja: Elsevier BV
Julkaisuvuosi: 2025
Lehti:: European Journal of Pharmaceutical Sciences
Artikkelin numero: 107310
Vuosikerta: 214
ISSN: 0928-0987
eISSN: 1879-0720
DOI: https://doi.org/10.1016/j.ejps.2025.107310
Verkko-osoite: https://doi.org/10.1016/j.ejps.2025.107310
Rinnakkaistallenteen osoite: https://research.utu.fi/converis/portal/detail/Publication/504680773
Acyclovir (ACV), an antiviral drug, belongs to the BCS class III drug with intermediate solubility and low permeability. The limited permeability leads to low drug absorption, making it poorly bioavailable. Consequently, to achieve the ACV concentration within the therapeutic range, frequent dosing is required which can lead to several side effects. Thus, increasing the permeability of ACV is critical for enhancing bioavailability, overall therapeutic outcomes and patient compliance. Advanced drug delivery systems (DDS), such as polymeric micelles, can be employed to enhance ACV bioavailability, as they offer distinct advantages. Notably, anionic polymeric micelles based on acid functionalized poly(jasmine lactone) copolymer were employed for the first time to improve ACV solubility and permeability. Micelles with size of approx. 100 nm were able to improve the aqueous solubility of ACV from 1.81 mg to 4.32 mg/mL. The anti-viral assay results reveal that ACV loaded micelles are equally effective in both prophylactic and therapeutic settings towards inhibiting herpes simplex virus type 1 compared to free ACV. The permeability study performed via phospholipid vesicle-based permeation assay (PVPA) indicated an improvement in ACV permeability when loaded in polymeric micelles compared to free ACV. This increase was observed both in absence as well as in the presence of an additional mucus layer. In silico simulations performed on GastroPlus® (GPX) software supported the outcomes of PVPA assay in a simulated human model. The obtained results indicated that negatively charged poly(jasmine lactone) micelles could significantly improve the therapeutic outcome of ACV by improving its solubility and oral permeability.
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This research was partly funded by Business Finland Research-to-Business project Jasmine PRO (1609/31/2021). J.V. acknowledges the funding support provided by National Overseas Scholarship, Ministry of Social Justice and Empowerment, Government of India, for her personal PhD scholarship, and the Swedish Cultural Foundation in Finland for a personal PhD grant (#199,427) and funding from NordForsk for the Nordic University Hub project #85,352 (Nordic POP, Patient Oriented Products) for providing the research mobility to perform the in vitro permeation study at UiT, The Arctic University of Norway, Tromsø, Norway. F.F. would further like to thank Åbo Akademi University Graduate School for personal funding in the form of PhD salary.
