Twin-screw extruded lipid implants containing TRP2 peptide for tumour therapy

Even, Marie-Paule; Bobbala, Sharan; Gibson, Blake; Hook, Sarah; Winter, Gerhard; Engert, Julia

doi:10.1016/j.ejpb.2016.12.033

Cited by 12 publications

(9 citation statements)

References 22 publications

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“…Production is nowadays most commonly based on holt melt extrusion (also named solid lipid extrusion), either in single-or twin-screw devices, a process that enables the achievement of a more sustained release and homogenous drug distribution in comparison to other methods. Often-encapsulated biologics are temperature-sensitive, so the lipid mixture must be carefully selected to ensure extrusion at lowest possible temperatures [151,[156][157][158]160]. Production by melting and casting lipid blends with drugs is no longer state of the art since it employs higher temperatures than those used in extrusion processes and could therefore cause instabilities in the APIs even faster [171,172].…”

Section: Solid Particles and Implantsmentioning

confidence: 99%

“…Production by melting and casting lipid blends with drugs is no longer state of the art since it employs higher temperatures than those used in extrusion processes and could therefore cause instabilities in the APIs even faster [171,172]. General insights into the effect of lipid composition and different preparation parameters on the physico-chemical characteristics and the in vitro release behavior (up to 28 weeks) were obtained using albumin or monoclonal antibodies as model proteins [156][157][158]160]. Lipid implants including a monoclonal antibody from the IgG 1 class and the f ab -fragment ranibizumab showed a sustained release in vitro of around 120 days with a good stability of the proteins, which were stabilized by cyclodextrines [151].…”

Section: Solid Particles and Implantsmentioning

confidence: 99%

“…Overall, recent studies mainly focus on the preparation and characterization of the implants and do not focus on the implementation in vivo and the drug release, pharmacokinetics, or pharmacodynamics. An exception is represented by Even and coworkers, who showed in vivo results using the tumor peptide TRP2 as an antigen in lipid implants [158]. The mice receiving this implant had a delayed tumor growth of three days compared to control groups without TRP2 treatment.…”

Section: Solid Particles and Implantsmentioning

confidence: 99%

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Injectable Lipid-Based Depot Formulations: Where Do We Stand?

Rahnfeld

Luciani

2020

Pharmaceutics

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The remarkable number of new molecular entities approved per year as parenteral drugs, such as biologics and complex active pharmaceutical ingredients, calls for innovative and tunable drug delivery systems. Besides making these classes of drugs available in the body, injectable depot formulations offer the unique advantage in the parenteral world of reducing the number of required injections, thus increasing effectiveness as well as patient compliance. To date, a plethora of excipients has been proposed to formulate depot systems, and among those, lipids stand out due to their unique biocompatibility properties and safety profile. Looking at the several long-acting drug delivery systems based on lipids designed so far, a legitimate question may arise: How far away are we from an ideal depot formulation? Here, we review sustained release lipid-based platforms developed in the last 5 years, namely oil-based solutions, liposomal systems, in situ forming systems, solid particles, and implants, and we critically discuss the requirements for an ideal depot formulation with respect to the used excipients, biocompatibility, and the challenges presented by the manufacturing process. Finally, we delve into lights and shadows originating from the current setups of in vitro release assays developed with the aim of assessing the translational potential of depot injectables.

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Section: Solid Particles and Implantsmentioning

confidence: 99%

Section: Solid Particles and Implantsmentioning

confidence: 99%

Section: Solid Particles and Implantsmentioning

confidence: 99%

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Injectable Lipid-Based Depot Formulations: Where Do We Stand?

Rahnfeld

Luciani

2020

Pharmaceutics

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“…Current vaccine development has focused on the use of purified subunit vaccines, which are regarded as offering better safety profiles than traditional vaccines based on live or attenuated organisms . However, subunit antigens suffer from poor immunogenicity and need to be administered multiple times along with potent adjuvants in order to stimulate effective immune responses . Sustained‐release delivery systems can deliver both the antigen and adjuvant for an extended period of time, facilitating an increased interaction time between the antigen and immune system, and subsequently increasing the possibility of an effective immune response .…”

Section: Introductionmentioning

confidence: 99%

“…1 However, subunit antigens suffer from poor immunogenicity and need to be administered multiple times along with potent adjuvants in order to stimulate effective immune responses. 2,3 Sustained-release delivery systems can deliver both the antigen and adjuvant for an extended period of time, facilitating an increased interaction time between the antigen and immune system, and subsequently increasing the possibility of an effective immune response. 4 However, concerns associated with sustained-release delivery systems such as tolerance and immune exhaustion need to be addressed.…”

Section: Introductionmentioning

confidence: 99%

Poloxamer 407‐chitosan grafted thermoresponsive hydrogels achieve synchronous and sustained release of antigen and adjuvant from single‐shot vaccines

et al. 2018

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Sustained-release vaccine delivery systems may enhance the immunogenicity of subunit vaccines and reduce the need for multiple vaccinations. The aim of this study was to develop a thermoresponsive hydrogel using poloxamer 407-chitosan (CP) grafted copolymer as a delivery system for single-shot sustained-release vaccines. The CP copolymer was synthesized using 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide and N-hydroxysuccinimide chemistry. The CP copolymer was a free flowing solution at ambient temperature and transformed rapidly into a gel at body temperature. The hydrogels were loaded with vaccine antigen and adjuvants or the vaccine components were encapsulated in poly (lactic-co-glycolic acid) nanoparticles in order to ensure synchronous release. The CP hydrogels were stable for up to 18 days in vitro. Release of both nanoparticles and the individual components was complete, with release of the individual components being modulated by incorporation into nanoparticles. In vivo, a single dose of CP hydrogel vaccine induced strong, long lasting, cellular and humoral responses that could protect against the development of tumors in a murine melanoma model.

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Twin-screw extrusion of sustained-release oral dosage forms and medical implants

Feng

Zhang

2017

Drug Deliv. and Transl. Res.

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Most of published reviews of twin-screw extrusion focused on its application for enhancing the bioavailability of amorphous solid dispersions while few of them focused on its use for manufacturing sustained-release oral dosage forms and medical implants, despite the considerable interest and success this process has garnered both in academia and in the pharmaceutical industry. Compared to conventional batch processing, twin-screw extrusion offers the advantages of continuous processing and the ability to prepare oral dosage forms and medical implants that have unique physicochemical and drug release attributes. This review provides an in-depth analysis of the formulation composition and processing conditions of twin-screw extrusion and how these factors affect the drug release properties of sustained-release dosage forms. This review also illustrates the unique advantages of this process by presenting case studies of a wide variety of commercial sustained-release products manufactured using twin-screw extrusion.

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Twin-screw extruded lipid implants containing TRP2 peptide for tumour therapy

Cited by 12 publications

References 22 publications

Injectable Lipid-Based Depot Formulations: Where Do We Stand?

Injectable Lipid-Based Depot Formulations: Where Do We Stand?

Poloxamer 407‐chitosan grafted thermoresponsive hydrogels achieve synchronous and sustained release of antigen and adjuvant from single‐shot vaccines

Twin-screw extrusion of sustained-release oral dosage forms and medical implants

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