Clinically established biodegradable long acting injectables: An industry perspective

Nkanga, Christian Isalomboto; Fisch, Andreas; Rad‐Malekshahi, Mazda; Romić, Marieta Duvnjak; Kittel, Birgit; Ullrich, Thomas; Wang, Jing; Krause, Rui Werner Maçedo; Adler, Sabine; Lammers, Twan; Hennink, Wim E.; Ramazani, Farshad

doi:10.1016/j.addr.2020.11.008

Cited by 103 publications

(41 citation statements)

References 288 publications

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“…While we have highlighted many successful examples of LAPFs ( Table 1 20 , 46 , 56 , 161 , 162 , 163 , 164 , 165 , 166 , 167 , 168 , 169 , 170 , 171 , 172 ), challenges still remain in many areas of their application. Improved technologies still need to solve the potential issues of current strategies.…”

Section: Future Perspectivesmentioning

confidence: 99%

“…Toward this end, a diverse array of strategies ( Fig. 1 ) has been developed to design LAPFs through endowing the therapeutic drugs with features that include slow and controlled release, delayed clearance, resistance to enzymes, increased stability, extended half-life 19 , 20 . By rationally designing, LAPFs are safer and more efficient.…”

Section: Introductionmentioning

confidence: 99%

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A review of existing strategies for designing long-acting parenteral formulations: Focus on underlying mechanisms, and future perspectives

Shi

Wang

et al. 2021

Acta Pharmaceutica Sinica B

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The need for long-term treatments of chronic diseases has motivated the widespread development of long-acting parenteral formulations (LAPFs) with the aim of improving drug pharmacokinetics and therapeutic efficacy. LAPFs have been proven to extend the half-life of therapeutics, as well as to improve patient adherence; consequently, this enhances the outcome of therapy positively. Over past decades, considerable progress has been made in designing effective LAPFs in both preclinical and clinical settings. Here we review the latest advances of LAPFs in preclinical and clinical stages, focusing on the strategies and underlying mechanisms for achieving long acting. Existing strategies are classified into manipulation of in vivo clearance and manipulation of drug release from delivery systems, respectively. And the current challenges and prospects of each strategy are discussed. In addition, we also briefly discuss the design principles of LAPFs and provide future perspectives of the rational design of more effective LAPFs for their further clinical translation.

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Section: Future Perspectivesmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

A review of existing strategies for designing long-acting parenteral formulations: Focus on underlying mechanisms, and future perspectives

Shi

Wang

et al. 2021

Acta Pharmaceutica Sinica B

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“…There is an increased frequency of administration of drugs that are susceptible to rapid in vivo clearance leading to poor patient compliance. Thus, development of controlled release strategies allows extended systemic exposure on administration of a single dose [44]. Key factors affecting drug release kinetics are variability in structure of the tissue, physiology of the recipient, rate of injection and technology format [45].…”

Section: Long-acting Injectable (Lai) Therapymentioning

confidence: 99%

“…LAI technology platforms include: (i) microencapsulation, (ii) in-situ forming depots (gels/implants) and (iii) molecular and particulate delivery systems. Invega Trinza ® and Invega Sustenna ® are sterile nanosuspensions of paliperidone palmitate that were first registered with a dose of 150 mg/human monthly and 525 mg/human every three months, respectively [44].…”

Section: Long-acting Injectable (Lai) Therapymentioning

confidence: 99%

Characterization and Applications of Colloidal Systems as Versatile Drug Delivery Carriers for Parenteral Formulations

2021

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Preparing a suitable formulation for parenteral administration is already a difficult task; this, coupled with poor water-soluble new chemical entity (NCE), complicates this situation even further. There are several methodologies available to enhance water solubility, but this alone does not entail successful formulation. Making a micro/nano emulsion with a suitable surfactant not only increases the drug solubility but also the cell membrane permeability. Thus, not only biopharmaceutic classification system (BCS)-II (low solubility compounds) but also BCS-III (low permeability) and BCS-IV drugs (low solubility and low permeability) can be further exploited. Those drug candidates otherwise will not move further in NCE evaluation or clinical trials. This succinct review article delves into various aspects of biphasic micro/nano emulsion systems for parenteral drug delivery including the structure of the biphasic colloidal systems, characterization parameters, stability issues, regulatory considerations, and applications in life sciences.

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“…In most cases, ISFD LAIs are designed using bioresorbable materials, which makes them ideal products to ensure long-term drug compliance by the patients while guaranteeing also an increased comfort. It is not surprising thus that several ISFD-based drug products have reached clinics for different indications and that many more are currently undergoing clinical trials [ 7 ].…”

Section: Introductionmentioning

confidence: 99%

Poly(ethylene glycol)-b-poly(1,3-trimethylene carbonate) Copolymers for the Formulation of In Situ Forming Depot Long-Acting Injectables

et al. 2021

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This article describes the utilization of (methoxy)poly(ethylene glycol)-b-poly(1,3-trimethylene carbonate) ((m)PEG–PTMC) diblock and triblock copolymers for the formulation of in situ forming depot long-acting injectables by solvent exchange. The results shown in this manuscript demonstrate that it is possible to achieve long-term drug deliveries from suspension formulations prepared with these copolymers, with release durations up to several months in vitro. The utilization of copolymers with different PEG and PTMC molecular weights affords to modulate the release profile and duration. A pharmacokinetic study in rats with meloxicam confirmed the feasibility of achieving at least 28 days of sustained delivery by using this technology while showing good local tolerability in the subcutaneous environment. The characterization of the depots at the end of the in vivo study suggests that the rapid phase exchange upon administration and the surface erosion of the resulting depots are driving the delivery kinetics from suspension formulations. Due to the widely accepted utilization of meloxicam as an analgesic drug for animal care, the results shown in this article are of special interest for the development of veterinary products aiming at a very long-term sustained delivery of this therapeutic molecule.

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Clinically established biodegradable long acting injectables: An industry perspective

Cited by 103 publications

References 288 publications

A review of existing strategies for designing long-acting parenteral formulations: Focus on underlying mechanisms, and future perspectives

A review of existing strategies for designing long-acting parenteral formulations: Focus on underlying mechanisms, and future perspectives

Characterization and Applications of Colloidal Systems as Versatile Drug Delivery Carriers for Parenteral Formulations

Poly(ethylene glycol)-b-poly(1,3-trimethylene carbonate) Copolymers for the Formulation of In Situ Forming Depot Long-Acting Injectables

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