Comparative Study of PLGA in-situ Implant and Nanoparticle Formulations of Entecavir; in-vitro and in-vivo evaluation

Ayoub, Margrit M.; Jasti, Bhaskara; Elantouny, Neveen G.; El-Nahas, Hanan M.; Ghazy, Fakhr-eldin S.

doi:10.1016/j.jddst.2020.101585

Cited by 10 publications

(9 citation statements)

References 42 publications

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“…Current attempts to design clinical therapies for viral infection usually inhibit viral replication using small-molecule drugs; nevertheless, their efficacy is limited by poor bioavailability, nontargeted release, and adverse side effects (35,36). Many kinds of delivery systems such as micelles, nanoliposomes, nanoemulsions, and biopolymer NPs can be designed to enhance the efficacy of antiviral drugs by overcoming the above obstacles (37)(38)(39). However, IAV infection activates the host's natural immune response.…”

Section: Discussionmentioning

confidence: 99%

Polydopamine-based nanomedicines for efficient antiviral and secondary injury protection therapy

Yin

Zhang

et al. 2023

Sci. Adv.

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Viral infections continue to threaten human health. It remains a major challenge to efficiently inhibit viral infection while avoiding secondary injury. Here, we designed a multifunctional nanoplatform (termed as ODCM), prepared by oseltamivir phosphate (OP)–loaded polydopamine (PDA) nanoparticles camouflaged by the macrophage cell membrane (CM). OP can be efficiently loaded onto the PDA nanoparticles through the π-π stacking and hydrogen bonding interactions with a high drug-loading rate of 37.6%. In particular, the biomimetic nanoparticles can accumulate actively in the damaged lung model of viral infection. At the infection site, PDA nanoparticles can consume excess reactive oxygen species and be simultaneously oxidized and degraded to achieve controlled release of OP. This system exhibits enhanced delivery efficiency, inflammatory storm suppression, and viral replication inhibition. Therefore, the system exerts outstanding therapeutic effects while improving pulmonary edema and protecting lung injury in a mouse model of influenza A virus infection.

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Section: Discussionmentioning

confidence: 99%

Polydopamine-based nanomedicines for efficient antiviral and secondary injury protection therapy

Yin

Zhang

et al. 2023

Sci. Adv.

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“…The authors also reported that encapsulation of the antiviral agent increased its ocular bioavailability compared to the free form. In another study, Ayoub, Jasti et al [ 12 ] showed that the antiviral agent entecavir could be encapsulated in PLGA nanoparticles and its release could be controlled by manipulating the formulation. The authors also used an in vivo study to show that the bioavailability of the entecavir was increased after encapsulation, which could lead to an effective approach for treating the hepatitis B virus.…”

Section: Nanoparticle Delivery Systems In Antiviral Therapymentioning

confidence: 99%

Development of nanoparticle-delivery systems for antiviral agents: A review

Delshadi¹,

Bahrami

McClements

et al. 2021

Journal of Controlled Release

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“…Hence, oral EV therapy is administered after fasting (2 h before or after a meal) as consumption with food might result in reduced exposure and lower efficacy 14 . Different LA injectable systems of EV such as microspheres, drug crystalline suspension, in situ implant, polymeric conjugate, liquid crystalline, and hot‐melt extrudate have been designed to better patient compliance with alleviated food effect on oral therapy 15–21 . We had previously synthesized entecavir‐3‐palmiate (EV‐P; Figure 1b), a lipidic ester prodrug in which fatty acids are covalently bound to the parent compound 16 .…”

Section: Introductionmentioning

confidence: 99%

“…14 Different LA injectable systems of EV such as microspheres, drug crystalline suspension, in situ implant, polymeric conjugate, liquid crystalline, and hot-melt extrudate have been designed to better patient compliance with alleviated food effect on oral therapy. [15][16][17][18][19][20][21] We had previously synthesized entecavir-3-palmiate (EV-P; Figure 1b), a lipidic ester prodrug in which fatty acids are covalently bound to the parent compound. 16 The covalent attachment of a fatty acid chain to EV markedly lowered their aqueous solubility, thus providing a sustained release of the lipidic prodrug.…”

Section: Introductionmentioning

confidence: 99%

Exploration of lipidic prodrug‐loaded oil depot system for intramuscular prolonged delivery of entecavir

Jeong

Choi

et al. 2023

Bulletin Korean Chem Soc

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Entecavir (EV) is a first‐line antiretroviral agent to treat chronic hepatitis B. However, its oral administration is challenging, due to food effect on intestinal absorption. Therefore, in order to afford improved patient's compliance, a novel long‐acting injectable oil depot (OD) system of entecavir‐3‐palmiate (EV‐P), a lipidic ester prodrug of EV, was formulated. The OD consisted of oleic acid and benzyl alcohol as oily vehicles, with a suitable viscosity (38.6 centipoise with shear rate of 1 s−1). The prodrug was gradually released from the OD under sink conditions, providing delayed liberation than that by the hydrophilic parent compound. Following the intramuscular injection in rats, EV‐P OD provided a markedly protracted EV profile compared to oral EV; the EV levels in plasma were expanded over 2 weeks, with elimination half‐life of about 7 days. Therefore, we concluded that EV‐P OD can be a promising approach for a prolonged delivery of EV.

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Comparative Study of PLGA in-situ Implant and Nanoparticle Formulations of Entecavir; in-vitro and in-vivo evaluation

Cited by 10 publications

References 42 publications

Polydopamine-based nanomedicines for efficient antiviral and secondary injury protection therapy

Polydopamine-based nanomedicines for efficient antiviral and secondary injury protection therapy

Development of nanoparticle-delivery systems for antiviral agents: A review

Exploration of lipidic prodrug‐loaded oil depot system for intramuscular prolonged delivery of entecavir

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