Spanlastics-Loaded Buccal Films for Improved Olmesartan Delivery and Sustained Hypertension Management: Formulation, Statistical Optimization, In Vitro and In Vivo Evaluation
Abstract
Abstract Purpose This study aimed to develop spanlastics-loaded buccal films to overcome the oral bioavailability limitations of olmesartan medoxomil (OLM), a sparsely water-soluble antihypertensive agent. Methods: OLM-loaded spanlastics were prepared using the ethanol injection method. A 2 4 factorial design was employed to investigate the effects of different variables on vesicles’ features and to identify the optimized spanlastic formula (OS). Vesicles were characterized in terms of entrapment efficiency (EE), particle size (PS), zeta potential (ZP), and polydispersity index (PDI). OS was further characterized in vitro, incorporated into buccal films, and its pharmacodynamic performance was assessed in a single-dose study in hypertensive rats, compared to orally administered OLM suspension. Results OS showed spherical vesicles with EE% of 67.7±2.97%, PS of 202.6±4.38 nm, ZP of ‒32.00±1.27 mV, and PDI of 0.272±0.00. OS showed markedly higher OLM release over 24 h compared to OLM suspension. Differential scanning calorimetry indicated drug amorphization. In vitro characterization, along with histopathological examination, demonstrated that OS-loaded films were well-tolerated and safe for buccal administration. Furthermore, pharmacodynamic evaluation revealed that these films significantly enhanced and sustained the antihypertensive effect of OLM, achieving a 1.68-fold increase in area under the antihypertensive effect-time curve and a 1.67-fold prolongation in effect…
Read the paper
Related studies
- Improving the translation of search strategies using the Polyglot Search Translator: a randomized controlled trial
- Nutritional, Physical, Cognitive, and Combination Interventions and Frailty Reversal Among Older Adults: A Randomized Controlled Trial
- Clinical characteristics and risk factors associated with COVID-19 severity in patients with haematological malignancies in Italy: a retrospective, multicentre, cohort study
- A randomized, controlled trial of oral propranolol in infantile hemangioma
- Clinical phenotypes of delirium during critical illness and severity of subsequent long-term cognitive impairment: a prospective cohort study
- Increased physical activity improves sleep and mood outcomes in inactive people with insomnia: a randomized controlled trial
Go deeper in Evidence Hub
Evidence Hub adds a study data sheet (design, sample size, evidence level, key numbers), an AI summary and a chat grounded in the paper's text.