Design of a long-term antipsychotic in situ forming implant and its release control method and mechanism

Wang, Lexi; Wang, Aiping; Zhao, Xiao-Lei; Liu, Ximing; Wang, Dan; Sun, Fengying; Li, Youxin

doi:10.1016/j.ijpharm.2012.02.015

Cited by 58 publications

(30 citation statements)

References 20 publications

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“…Typically, the rapid solvent extraction was often followed by a fast drug release. On the other hand, for the drugs of poor solubility, a rapid diffusion of DMSO would lead to a fast solidification of the implant, resulting in a high drug retention rate with prolongation of drug release [48]. Therefore, the aqueous diffusion and solvent exchange played the important role on drug release.…”

Section: Rate Of Water Diffusion Into the Gelsmentioning

confidence: 99%

In situ forming gel comprising bleached shellac loaded with antimicrobial drugs for periodontitis treatment

2016

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Section: Rate Of Water Diffusion Into the Gelsmentioning

confidence: 99%

In situ forming gel comprising bleached shellac loaded with antimicrobial drugs for periodontitis treatment

2016

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“…Typically, the rapid solvent extraction was often followed by a fast drug release. On the other hand, for the drugs of poor water solubility, a rapid diffusion of DMSO would lead to a fast solidification of the implant, resulting in a high drug retention rate with prolongation of drug release (39). Therefore, the aqueous diffusion and solvent exchange also played an important role on drug release.…”

Section: Rate Of Water Diffusion Into Gelsmentioning

confidence: 99%

Characterization of Antimicrobial Agent Loaded Eudragit RS Solvent Exchange-Induced In Situ Forming Gels for Periodontitis Treatment

et al. 2016

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Eudragit RS (ERS), a quaternary polyacrylate positively charged polymer, exhibits a very low permeability and swells in aqueous media independently of pH without dissolving. Owing to its high solubility in N-methyl pyrrolidone (NMP), it was interesting to apply as polymer matrix for solvent-exchanged in situ forming gel. The aim of this research was to prepare in situ forming gels from ERS to deliver the antimicrobial agents (doxycycline hyclate, metronidazole, and benzoyl peroxide) for periodontitis treatment. They were evaluated for viscosity and rheology, gel formation, syringeability, drug release, and antimicrobial activities. The solvent exchange between NMP and an external aqueous simulated gingival crevicular fluid stimulated the dissolved ERS transforming into the opaque rigid gel. Antimicrobial agent loaded ERS systems exhibited Newtonian flow with acceptable syringeability. The higher-loaded ERS promoted the more prolongation of drug release because of the retardation of water diffusion into the precipitated matrix. Antimicrobial activities against Staphylococcus aureus, Escherichia coli, Candida albicans, Streptococcus mutans, and Porphyromonas gingivalis depended on type of drugs and test microorganisms. Doxycycline hyclate loaded ERS systems showed these activities greater than the others; however, all of them could inhibit all test microorganisms. Thus, the solvent exchange-induced in situ forming gels comprising ERS-antimicrobial drugs exhibited potential use as localized delivery systems for periodontitis treatment.

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“…The diffusion rate of the aqueous phosphate buffer pH 7.2 into the polymeric solutions decreased with increasing the triblock polymer concentration (P,0.05; Figure 5) due to the increased gel viscosity. Wang et al 28 demonstrated that the fast partitioning of the employed solvent might cause fast solidification of the implant; hence, higher drug retention rate was expected. Glimepiride release from the prepared gels was conducted in phosphate buffer pH 7.2 to simulate the physiologic condition ( Figure 5).…”

Section: Characterization Of the Prepared In Situ Gelsmentioning

confidence: 99%

Mechanistic analysis of Zein nanoparticles/PLGA triblock in situ forming implants for glimepiride

Ahmed¹,

Zidan²,

Khayat³

2016

IJN

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Objectives The study aims at applying pharmaceutical nanotechnology and D-optimal fractional factorial design to screen and optimize the high-risk variables affecting the performance of a complex drug delivery system consisting of glimepiride–Zein nanoparticles and inclusion of the optimized formula with thermoresponsive triblock copolymers in in situ gel. Methods Sixteen nanoparticle formulations were prepared by liquid–liquid phase separation method according to the D-optimal fractional factorial design encompassing five variables at two levels. The responses investigated were glimepiride entrapment capacity (EC), particle size and size distribution, zeta potential, and in vitro drug release from the prepared nanoparticles. Furthermore, the feasibility of embedding the optimized Zein-based glimepiride nanoparticles within thermoresponsive triblock copolymers poly(lactide- co -glycolide)-block-poly(ethylene glycol)-block-poly(lactide- co -glycolide) in in situ gel was evaluated for controlling glimepiride release rate. Results Through the systematic optimization phase, improvement of glimepiride EC of 33.6%, nanoparticle size of 120.9 nm with a skewness value of 0.2, zeta potential of 11.1 mV, and sustained release features of 3.3% and 17.3% drug released after 2 and 24 hours, respectively, were obtained. These desirability functions were obtained at Zein and glimepiride loadings of 50 and 75 mg, respectively, utilizing didodecyldimethylammonium bromide as a stabilizer at 0.1% and 90% ethanol as a common solvent. Moreover, incorporating this optimized formulation in triblock copolymers-based in situ gel demonstrated pseudoplastic behavior with reduction of drug release rate as the concentration of polymer increased. Conclusion This approach to control the release of glimepiride using Zein nanoparticles/triblock copolymers-based in situ gel forming intramuscular implants could be useful for improving diabetes treatment effectiveness.

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Design of a long-term antipsychotic in situ forming implant and its release control method and mechanism

Cited by 58 publications

References 20 publications

In situ forming gel comprising bleached shellac loaded with antimicrobial drugs for periodontitis treatment

In situ forming gel comprising bleached shellac loaded with antimicrobial drugs for periodontitis treatment

Characterization of Antimicrobial Agent Loaded Eudragit RS Solvent Exchange-Induced In Situ Forming Gels for Periodontitis Treatment

Mechanistic analysis of Zein nanoparticles/PLGA triblock in situ forming implants for glimepiride

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