In situ Formed Implants, Based on PLGA and Eudragit Blends, for Novel Florfenicol Controlled Release Formulations

Karp, Federico; Turino, Ludmila Noelia; Helbling, Ignacio Marcelo; Islan, Germán Abel; Luna, Julio Alberto; Estenoz, Diana Alejandra

doi:10.1016/j.xphs.2020.11.006

Cited by 14 publications

(4 citation statements)

References 44 publications

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“…Eudragit S100 (ES100) is a pH-sensitive synthetic polymer of which the upper limit of the pH threshold is 7. Since 2010, it has had increasingly wide application in drug industries [ 24 , 25 ]. ES100 is promising in delivering drugs because it is not only insoluble in aqueous media but also nontoxic, nonirritant, biocompatible and permeable, which make drug release controllable.…”

Section: Introductionmentioning

confidence: 99%

One-Pot Self-Assembly of Core-Shell Nanoparticles within Fibers by Coaxial Electrospinning for Intestine-Targeted Delivery of Curcumin

Hou

Zhang

et al. 2023

Foods

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Nanotechniques for curcumin (Cur) encapsulation provided a potential capability to avoid limitations and improve biological activities in food and pharmaceutics. Different from multi-step encapsulation systems, in this study, zein–curcumin (Z–Cur) core-shell nanoparticles could be self-assembled within Eudragit S100 (ES100) fibers through one-pot coaxial electrospinning with Cur at an encapsulation efficiency (EE) of 96% for ES100–zein–Cur (ES100–Z–Cur) and EE of 67% for self-assembled Z–Cur. The resulting structure realized the double protection of Cur by ES100 and zein, which provided both pH responsiveness and sustained release performances. The self-assembled Z–Cur nanoparticles released from fibermats were spherical (diameter 328 nm) and had a relatively uniform distribution (polydispersity index 0.62). The spherical structures of Z–Cur nanoparticles and Z–Cur nanoparticles loaded in ES100 fibermats could be observed by transmission electron microscopy (TEM). Fourier transform infrared spectra (FTIR) and X-ray diffractometer (XRD) revealed that hydrophobic interactions occurred between the encapsulated Cur and zein, while Cur was amorphous (rather than in crystalline form). Loading in the fibermat could significantly enhance the photothermal stability of Cur. This novel one-pot system much more easily and efficiently combined nanoparticles and fibers together, offering inherent advantages such as step economy, operational simplicity, and synthetic efficiency. These core-shell biopolymer fibermats which incorporate Cur can be applied in pharmaceutical products toward the goals of sustainable and controllable intestine-targeted drug delivery.

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Section: Introductionmentioning

confidence: 99%

One-Pot Self-Assembly of Core-Shell Nanoparticles within Fibers by Coaxial Electrospinning for Intestine-Targeted Delivery of Curcumin

Hou

Zhang

et al. 2023

Foods

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“…Upon addition to an aqueous solution, the solvent is removed from the polymer, resulting in a semisolid matrix that entraps the drug compound. Over time, the many drugs are released through diffusion and progressive polymer degradation [ 20 , 21 , 22 ]. An ideal in situ gel former should possess low water solubility but can dissolve in water-miscible organic solvents [ 23 ].…”

Section: Introductionmentioning

confidence: 99%

Injectable Gamboge-Based In Situ Gel for Sustained Delivery of Imatinib Mesylate

Jitrangsri,

Khaing,

Intaraphairot

et al. 2023

Gels

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The aim of this study was to prepare and characterize the imatinib mesylate (IM)-loaded gamboge-based ISG system for local administration of an anticancer agent against colorectal carcinoma. The ISG formulations were prepared in dimethyl sulfoxide (DMSO) and N-methyl-2-pyrrolidone (NMP). The physicochemical properties, drug release profile, and cytotoxicity of the developed formulations were assessed. The developed ISG demonstrated Newtonian flow behavior with acceptable rheological and mechanical properties. The viscosity of the developed ISG, measured at less than 80 cP, and the applied forces of less than 50 N·mm, indicated easy administration using clinical injection techniques. Upon contact with an aqueous phase, the ISG immediately formed a porous cross-sectional structure, enabling sustained release of IM over 14 days. The release profile of IM was fitted to the quasi-Fickian diffusion mechanism, and the release rate could be controlled by the types of solvent and the amount of IM content. The developed IM-loaded gamboge ISG effectively inhibited colorectal cancer cells, including HCT116 and HT29 cell lines, with less than 20% cell viability observed at a concentration of 1% w/w IM after 2 days of incubation. This suggests that the developed ISG may potentially serve as an injectable system for localized anticancer delivery against colorectal cells, potentially reducing the side effects of systemic chemotherapy and improving patient adherence.

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“…The researchers hypothesised that the solubility of Eudragit ® E100 increases at low pH values, leading to destabilisation of the polymer implants. On the other hand, Eudragit ® S100 loses its solubility in an acidic environment, maintaining the composition of the polymer matrix [ 59 ].…”

Section: Possible Causes Of the “Burst Release” Problemmentioning

confidence: 99%

Burst Release from In Situ Forming PLGA-Based Implants: 12 Effectors and Ways of Correction

Bakhrushina,

Sakharova,

Konogorova

et al. 2024

Pharmaceutics

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In modern pharmaceutical technology, modified-release dosage forms, such as in situ formed implants, are gaining rapidly in popularity. These dosage forms are created based on a configurable matrix consisting of phase-sensitive polymers capable of biodegradation, a hydrophilic solvent, and the active substance suspended or dissolved in it. The most used phase-sensitive implants are based on a biocompatible and biodegradable polymer, poly(DL-lactide-co-glycolide) (PLGA). Objective: This systematic review examines the reasons for the phenomenon of active ingredient “burst” release, which is a major drawback of PLGA-based in situ formed implants, and the likely ways to correct this phenomenon to improve the quality of in situ formed implants with a poly(DL-lactide-co-glycolide) matrix. Data sources: Actual and relevant publications in PubMed and Google Scholar databases were studied. Study selection: The concept of the review was based on the theory developed during literature analysis of 12 effectors on burst release from in situ forming implants based on PLGA. Only those studies that sufficiently fully disclosed one or another component of the theory were included. Results: The analysis resulted in development of a systematic approach called the “12 Factor System”, which considers various constant and variable, endogenous and exogenous factors that can influence the nature of ‘burst release’ of active ingredients from PLGA polymer-based in situ formed implants. These factors include matrix porosity, polymer swelling, LA:GA ratio, PLGA end groups, polymer molecular weight, active ingredient structure, polymer concentration, polymer loading with active ingredients, polymer combination, use of co-solvents, addition of excipients, and change of dissolution conditions. This review also considered different types of kinetics of active ingredient release from in situ formed implants and the possibility of using the “burst release” phenomenon to modify the active ingredient release profile at the site of application of this dosage form.

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In situ Formed Implants, Based on PLGA and Eudragit Blends, for Novel Florfenicol Controlled Release Formulations

Cited by 14 publications

References 44 publications

One-Pot Self-Assembly of Core-Shell Nanoparticles within Fibers by Coaxial Electrospinning for Intestine-Targeted Delivery of Curcumin

One-Pot Self-Assembly of Core-Shell Nanoparticles within Fibers by Coaxial Electrospinning for Intestine-Targeted Delivery of Curcumin

Injectable Gamboge-Based In Situ Gel for Sustained Delivery of Imatinib Mesylate

Burst Release from In Situ Forming PLGA-Based Implants: 12 Effectors and Ways of Correction

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