UTILIZATION OF LYOPHILIZED LECIPLEXFOR AUGMENTING THE ORAL DELIVERY OF TENOFOVIR ALAFENAMIDE FUMARATE; STATISTICAL DESIGN, AND PHARMACOKINETIC EVALUATION

Authors

  • ALI SAEED OWAYEZ ALJABERI Faculty of Pharmacy, Cairo University, Giza Governorate 3750210, Egypt. Department of Pharmacy, Mazaya University College, Nasiriyah, Dhi Qar Governorate, Iraq
  • SARA NAGEEB EL-HELALY Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street-11562 Cairo, Egypt.
  • MINA I. TADROS Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street-11562 Cairo, Egypt. Department of Pharmaceutics, Faculty of Pharmacy and Drug Technology, Egyptian Chinese University, Cairo, Egypt
  • NERMEEN A. ELKASABGY Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street-11562 Cairo, Egypt

DOI:

https://doi.org/10.22159/ijap.2026v18i4.58365

Keywords:

Leciplex, Tenofovir alafenamide fumarate, Antiviral, D-optimal design, In vivo study

Abstract

Objective: This study aims to fabricate an oral drug delivery approach of tenofovir alafenamide fumarate (TAF) for managing viral infection using TAF-loaded leciplex.

Methods: Leciplex was assembled via a single one-step method and optimized via D-optimal design. The leciplex was characterized by its entrapment efficiency (EE%), vesicle size (VS), polydispersity index (PDI), and zeta potential (ZP). The optimum leciplex formulation consisted of 1:1.5 phospholipid G90: cetyltrimethylammonium bromide (CTAB).

Results: The optimum leciplex possessed VS, PDI, EE%, and ZP of 318.00±14.06 nm, 0.477±0.005, 90.45±1.03% and28.00 ± 1.20 mV, respectively. The optimum leciplex was lyophilized using mannitol then characterized, where no significant difference was revealed compared to optimum leciplex. The in vitro release assessment showed an enhanced release profile from the optimum lyophilized leciplex compared to the TAF suspension. The scanning electron microscope proved the alteration of TAF to an amorphous form within the optimum lyophilized TAF-loaded leciplex construction. The effect of storage at 4±0.5 ℃ suggested the maintenance of the optimum lyophilized leciplex integrity for up to three months. The pharmacokinetic study using male Albino rabbits showed that the optimum lyophilized leciplex possessed significantly higher Cmax and AUC0–24values relative to TAF capsule, with a relative bioavailability equals to 235.12%.

Conclusion: These results established the capability of optimum lyophilized TAF-loaded leciplex as a nanosystem for treating viral infections.

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doi: 10.3390/pharmaceutics14102215.

Published

2026-05-20

How to Cite

ALJABERI, A. S. O., EL-HELALY, S. N., TADROS, M. I., & ELKASABGY, N. A. (2026). UTILIZATION OF LYOPHILIZED LECIPLEXFOR AUGMENTING THE ORAL DELIVERY OF TENOFOVIR ALAFENAMIDE FUMARATE; STATISTICAL DESIGN, AND PHARMACOKINETIC EVALUATION. International Journal of Applied Pharmaceutics, 18(4). https://doi.org/10.22159/ijap.2026v18i4.58365

Issue

Articles In Press [Jul-Aug 2026]

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Original Article(s)

Copyright (c) 2026 ALI SAEED OWAYEZ ALJABERI, SARA NAGEEB EL-HELALY, MINA I. TADROS, NERMEEN A. ELKASABGY

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