Spanlastics-Loaded Buccal Films for Improved Olmesartan Delivery and Sustained Hypertension Management: Formulation, Statistical Optimization, In Vitro and In Vivo Evaluation

Q: What are the key findings of this study?

Olmesartan spanlastics-loaded buccal films increased the antihypertensive effect-time curve area by 1.68-fold and prolonged effect half-life by 1.67-fold vs oral suspension in hypertensive rats.

Q: What is the clinical evidence from this study?

Population: Dexamethasone-induced hypertension (animal model) (n=24). Intervention: Olmesartan medoxomil (OLM) spanlastics-loaded mucoadhesive buccal film vs. Oral olmesartan medoxomil suspension (10 mg/kg in deionized water), untreated hypertensive control, and normotensive control. Primary outcome: Area under the antihypertensive effect-time curve from 0 to 48 hours (AUEC0-48) and effect half-life (T1/2) based on percentage blood pressure reduction (1.68-fold increase in AUEC0-48 and 1.67-fold prolongation in effect half-life, p=<0.05).

Q: What question did this study set out to answer?

To develop and optimize spanlastics-loaded buccal films to overcome the low oral bioavailability of olmesartan medoxomil and achieve sustained antihypertensive efficacy.

Amira N. Abd Elrady; Mona Mohamed Elkhatib; Magdy I. Mohamed; Ahmed M. Fatouh

doi:10.1007/s12247-025-10347-3

January 29, 2026Journal of Pharmaceutical InnovationOpen Access

Spanlastics-Loaded Buccal Films for Improved Olmesartan Delivery and Sustained Hypertension Management: Formulation, Statistical Optimization, In Vitro and In Vivo Evaluation

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Key result

Buccal olmesartan films increase antihypertensive effect area ~68% vs oral suspension in hypertensive rats.

1.68-fold increase in AUEC0-48 and 1.67-fold prolongation in effect half-life
P<0.05
n=24

Key Points

To develop and optimize spanlastics-loaded buccal films to overcome the low oral bioavailability of olmesartan medoxomil and achieve sustained antihypertensive efficacy.
Prepared olmesartan-loaded spanlastics using the ethanol injection method and a 2^4 factorial design to determine an optimized spanlastic formulation based on vesicle characteristics.
Incorporated the optimized formula into buccal films, evaluated mucosal tolerance via histopathology in six New Zealand rabbits, and tested pharmacodynamics across 48 h in 24 male Wistar rats compared to an oral suspension.
The optimized spanlastic formula produced spherical vesicles with an entrapment efficiency of 67.7±2.97%, particle size of 202.6±4.38 nm, zeta potential of ‒32.00±1.27 mV, and polydispersity index of 0.272±0.00.
In hypertensive rats, the optimized buccal film achieved a 1.68-fold increase in the area under the antihypertensive effect-time curve (AUEC0–48) and a 1.67-fold prolongation in effect half-life compared to oral drug suspension.

PICO

P

Population

24 adult male Wistar rats (18 with dexamethasone-induced hypertension and 6 normotensive controls) evaluated over 48 hours following a single dose, plus 6 male New Zealand white rabbits for 8-hour mucosal safety histopathology.

I

Intervention / Comparator

Olmesartan medoxomil (OLM) spanlastics-loaded mucoadhesive buccal film vs Oral olmesartan medoxomil suspension (10 mg/kg in deionized water), untreated hypertensive control, and normotensive control (10 mg/kg equivalent of olmesartan medoxomil (single dose))

O

Primary Outcome

Area under the antihypertensive effect-time curve from 0 to 48 hours (AUEC0-48) and effect half-life (T1/2) based on percentage blood pressure reduction — 1.68-fold increase in AUEC0-48 and 1.67-fold prolongation in effect half-life, p=<0.05

Main Result

Effect estimate: 1.68-fold increase in AUEC0-48 and 1.67-fold prolongation in effect half-life

p-value: p=<0.05

Limitations

Preclinical animal study conducted in rats and rabbits without human clinical testing
Small sample size (n=6 rats per group in the pharmacodynamic study and n=3 rabbits per group in the histopathological study)
Single-dose evaluation over 48 hours without long-term chronic dosing assessment

Implication

Reveals enhanced antihypertensive effects of olmesartan delivered via spanlastics-loaded buccal films, indicating a promising delivery method.

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 half-life. Conclusion These findings confirm the enhanced and sustained antihypertensive effect of OLM delivered via spanlastics-loaded buccal films, highlighting them as a promising delivery system for OLM.

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Cite This Study

Elrady et al. (2026) studied Dexamethasone-induced hypertension (animal model) (n=24). Olmesartan medoxomil (OLM) spanlastics-loaded mucoadhesive buccal film vs. Oral olmesartan medoxomil suspension (10 mg/kg in deionized water), untreated hypertensive control, and normotensive control was evaluated on Area under the antihypertensive effect-time curve from 0 to 48 hours (AUEC0-48) and effect half-life (T1/2) based on percentage blood pressure reduction (1.68-fold increase in AUEC0-48 and 1.67-fold prolongation in effect half-life, p=<0.05). Olmesartan spanlastics-loaded buccal films increased the antihypertensive effect-time curve area by 1.68-fold and prolonged effect half-life by 1.67-fold vs oral suspension in hypertensive rats.

synapsesocial.com/papers/6980fd18c1c9540dea80ed76 https://doi.org/10.1007/s12247-025-10347-3

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Spanlastics-Loaded Buccal Films for Improved Olmesartan Delivery and Sustained Hypertension Management: Formulation, Statistical Optimization, In Vitro and In Vivo Evaluation

Key Points

PICO

Main Result

Limitations

Implication

Abstract

Discussion

Cite This Study

Spanlastics-Loaded Buccal Films for Improved Olmesartan Delivery and Sustained Hypertension Management: Formulation, Statistical Optimization, In Vitro and In Vivo Evaluation

Key Points

PICO

Main Result

Limitations

Implication

Abstract

Discussion

Cite This Study

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