In situ forming implants — an attractive formulation principle for parenteral depot formulations

Kempe, Sabine; Mäder, Karsten

doi:10.1016/j.jconrel.2012.04.016

Cited by 249 publications

(180 citation statements)

References 138 publications

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“…Morphological characterization of such systems has revealed that these depots possess a smaller pore size and are homogeneously dense. The main drawback of these solutions is their viscosity which makes them difficult to inject without previous warming to 37 °C [5].…”

Section: Use Of Hydrophobic Solventsmentioning

confidence: 99%

“…In situ gel (ISG) systems have been introduced in recent decades for the purpose of drug delivery and injectable tissue engineering [2,3]. In tissue engineering, a biocompatible system is employed to repair or replace portions of tissue or whole tissues such as bone, cartilage, blood vessels, skin, muscle, etc., while their use in drug delivery is mainly directed at controlling and sustaining the release of the administered drug [4,5].…”

Section: Introductionmentioning

confidence: 99%

“…Among the aforementioned mechanisms, in situ polymer precipitation based on the process of solvent removal or exchange is common and has been developed into commercially available products [5]. Leuprolide acetate, doxycycline hyclate, bupivacaine, risperidone and paclitaxel are common examples of drugs commercially available or in clinical trials as in situ forming implants [5].…”

Section: Introductionmentioning

confidence: 99%

“…Leuprolide acetate, doxycycline hyclate, bupivacaine, risperidone and paclitaxel are common examples of drugs commercially available or in clinical trials as in situ forming implants [5].…”

Section: Introductionmentioning

confidence: 99%

See 3 more Smart Citations

Preparation of Parenteral in situ Gel Formulation Based on smart PLGA polymer: Concepts to Decrease Initial Drug Burst and extend drug release

Ahmed¹,

Hussain²

2017

Biodegradable Polymers: Recent Developments and New Perspectives

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Section: Use Of Hydrophobic Solventsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

“…Leuprolide acetate, doxycycline hyclate, bupivacaine, risperidone and paclitaxel are common examples of drugs commercially available or in clinical trials as in situ forming implants [5].…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Preparation of Parenteral in situ Gel Formulation Based on smart PLGA polymer: Concepts to Decrease Initial Drug Burst and extend drug release

Ahmed¹,

Hussain²

2017

Biodegradable Polymers: Recent Developments and New Perspectives

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“…The organogel, however, could be injected through syringe needle with the aid of ''gelation inhibitor'', which belongs to some of the amphiphilic solvents. N-methyl-2-pyrrolodone (NMP) involved in the commercialization of a PLGA-based injectable implant (Eligard Õ ), is found to disrupt the organogel blocks and then facilitate the injection (Oliver, 2003;Kempe & Mäder, 2012). Upon injection, NMP would diffuse into the surrounding tissues and allow the in situ formation of the organogel implant without irreversible gel damage.…”

Section: Introductionmentioning

confidence: 99%

Self-assembled drug delivery system based on low-molecular-weight bis-amide organogelator: synthesis, properties and in vivo evaluation

Cao

et al. 2016

Drug Delivery

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(2016) Self-assembled drug delivery system based on low-molecular-weight bisamide organogelator: synthesis, properties and invivo evaluation, Drug Delivery, 23:8, 3168-3178, DOI: 10.3109/10717544.2016 RESEARCH ARTICLESelf-assembled drug delivery system based on low-molecular-weight bis-amide organogelator: synthesis, properties and in vivo evaluation Zhen Li, Jinxu Cao, Heran Li, Hongzhuo Liu, Fei Han, Zhenyun Liu, Chao Tong, and Sanming Li School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning, P.R. China Abstract Context: Orgnaogels based on amino acid derivatives have been widely used in the area of drug delivery. Objective: An organogel system based on L-lysine derivatives was designed and prepared to induce a thermal sensitive implant with higher transition temperature, better mechanical strength, and shorter gelation time. Materials and methods: The organogel was prepared by injectable soybean oil and methyl (S)-2,5-ditetradecanamidopentanoate (MDP), which was synthesized for the first time. Candesartan cilexetil (CC) was chosen as model drug. Different formulations were designed and optimized by response surface method. Thermal, rheology properties, and gelation kinetics of the optimized formulation had been characterized. The release behaviors in vitro, as well as in vivo were evaluated in comparison with the oily solution of drugs. Finally, the local inflammation response of in situ organogel was assessed by histological analysis. Results and discussion: Results showed that the synthesized gelator, MDP, had a good gelation ability and the organogels obtained via the self-assembly of gelators in vegetable oils exhibited great thermal and rheology properties, which guaranteed their state in body. In vivo pharmacokinetic demonstrated that the organogel formulation could extend the drug release and maintain a therapeutically effective plasma concentration at least 10 d. In addition, this implant showed acceptable moderate inflammation. Conclusion: The in situ forming L-lysine-derivative-based organogel could be a promising matrix for sustained drug delivery of the drugs with low solubility. KeywordsBiocompatibility, gelator, in situ implant system, in vivo release, organogel History

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Alternative Solid Forms: Salts

Stahl¹,

Sutter

Grandeury

et al. 2018

Polymorphism in the Pharmaceutical Industry

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In situ forming implants — an attractive formulation principle for parenteral depot formulations

Cited by 249 publications

References 138 publications

Preparation of Parenteral in situ Gel Formulation Based on smart PLGA polymer: Concepts to Decrease Initial Drug Burst and extend drug release

Preparation of Parenteral in situ Gel Formulation Based on smart PLGA polymer: Concepts to Decrease Initial Drug Burst and extend drug release

Self-assembled drug delivery system based on low-molecular-weight bis-amide organogelator: synthesis, properties and in vivo evaluation

Alternative Solid Forms: Salts

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