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Volume 17
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Article

pH-Sensitive In Situ Gel of Mirtazapine Invasomes for Rectal Drug Delivery: Protruded Bioavailability and Anti-Depressant Efficacy

by
Essam M. Eissa
1,
Amani M. El Sisi
1,
Marina A. Bekhet
1,
Fatma I. Abo El-Ela
2,
Rasha M. Kharshoum
1,
Adel A. Ali
1,
Majed Alrobaian
3 and
Ahmed M. Abdelhaleem Ali
3,*
1
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni-Suef University, Beni-Suef 62514, Egypt
2
Department of Pharmacology, Faculty of Veterinary Medicine, Beni-Suef University, Beni-Suef 62511, Egypt
3
Department of Pharmaceutics and Industrial Pharmacy, College of Pharmacy, Taif University, Taif 21944, Saudi Arabia
*
Author to whom correspondence should be addressed.
Pharmaceuticals 2024, 17(8), 978; https://doi.org/10.3390/ph17080978
Submission received: 18 June 2024 / Revised: 4 July 2024 / Accepted: 17 July 2024 / Published: 24 July 2024
(This article belongs to the Special Issue Pharmaceutical Formulation Characterization Design)
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Abstract

The present research emphasizes fabrication alongside the assessment of an innovative nano-vesicular membranous system known as invasomes (NVMs) laden with Mirtazapine for rectal administration. This system could circumvent the confines of orally administered counterparts regarding dose schedules and bioavailability. Mirtazapine invasomes were tailored by amalgamating phospholipid, cineole, and ethanol through a thin-film hydration approach rooted in the Box–Behnken layout. Optimization of composition parameters used to fabricate desired NVMs’ physicochemical attributes was undertaken using the Design-Expert® program. The optimal MRZ-NVMs were subsequently transformed to a pH-triggered in situ rectal gel followed by animal pharmacodynamic and pharmacokinetic investigations relative to rectal plain gel and oral suspension. The optimized NVMs revealed a diameter size of 201.3 nm, a z potential of −28.8 mV, an entrapment efficiency of 81.45%, a cumulative release within 12 h of 67.29%, and a cumulative daily permeated quantity of 468.68 µg/cm2. Compared to the oral suspension, pharmacokinetic studies revealed a 2.85- and 4.45-fold increase in calculated rectal bioavailability in circulation and brain, respectively. Pharmacodynamic and immunohistopathology evaluations exposed superior MRZ-NVMs attributed to the orally administered drug. Consequently, rectal MRZ-NVMs can potentially be regarded as a prospective nanoplatform with valuable pharmacokinetics and tolerability assets.
Keywords: depression; invasomes; pharmacokinetics; pharmacodynamics; rectal delivery depression; invasomes; pharmacokinetics; pharmacodynamics; rectal delivery
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MDPI and ACS Style

Eissa, E.M.; El Sisi, A.M.; Bekhet, M.A.; El-Ela, F.I.A.; Kharshoum, R.M.; Ali, A.A.; Alrobaian, M.; Ali, A.M.A. pH-Sensitive In Situ Gel of Mirtazapine Invasomes for Rectal Drug Delivery: Protruded Bioavailability and Anti-Depressant Efficacy. Pharmaceuticals 2024, 17, 978. https://doi.org/10.3390/ph17080978

AMA Style

Eissa EM, El Sisi AM, Bekhet MA, El-Ela FIA, Kharshoum RM, Ali AA, Alrobaian M, Ali AMA. pH-Sensitive In Situ Gel of Mirtazapine Invasomes for Rectal Drug Delivery: Protruded Bioavailability and Anti-Depressant Efficacy. Pharmaceuticals. 2024; 17(8):978. https://doi.org/10.3390/ph17080978

Chicago/Turabian Style

Eissa, Essam M., Amani M. El Sisi, Marina A. Bekhet, Fatma I. Abo El-Ela, Rasha M. Kharshoum, Adel A. Ali, Majed Alrobaian, and Ahmed M. Abdelhaleem Ali. 2024. "pH-Sensitive In Situ Gel of Mirtazapine Invasomes for Rectal Drug Delivery: Protruded Bioavailability and Anti-Depressant Efficacy" Pharmaceuticals 17, no. 8: 978. https://doi.org/10.3390/ph17080978

APA Style

Eissa, E. M., El Sisi, A. M., Bekhet, M. A., El-Ela, F. I. A., Kharshoum, R. M., Ali, A. A., Alrobaian, M., & Ali, A. M. A. (2024). pH-Sensitive In Situ Gel of Mirtazapine Invasomes for Rectal Drug Delivery: Protruded Bioavailability and Anti-Depressant Efficacy. Pharmaceuticals, 17(8), 978. https://doi.org/10.3390/ph17080978

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