A Uniform Ultra-Small Microsphere/SAIB Hybrid Depot with Low Burst Release for Long-Term Continuous Drug Release

Xia, Lin; Xu, Yuhong; Tang, Xing; Zhang, Yan; Chen, Jian; Zhang, Yu; He, Huan; Yang, Ziyi

doi:10.1007/s11095-015-1731-1

Cited by 16 publications

(14 citation statements)

References 40 publications

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“…Lin et al. (2015) demonstrated that combining PLGA microspheres with SAIB depots could reduce the burst release of risperidone to 0.64% after 1 day.…”

Section: Introductionmentioning

confidence: 99%

Electrosprayed naringin-loaded microsphere/SAIB hybrid depots enhance bone formation in a mouse calvarial defect model

et al. 2019

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The burst release of active osteogenic factors, which is not beneficial to osteogenesis, is commonly encountered in bone tissue engineering. The aims of this study were to prepare naringin-loaded microsphere/sucrose acetate isobutyrate (Ng-m-SAIB) hybrid depots, reduce the burst release of naringin (Ng), and improve osteogenesis. The morphology and size distributions of electrosprayed Ng-microspheres were characterized by scanning electron microscopy (SEM). The Ng-microspheres and Ng-m-SAIB depots were characterized by Fourier transform infrared spectroscopy (FTIR) and in vitro release studies. In vitro osteoblast-microsphere interactions and in vivo osteogenesis were assessed after implantation of Ng-m-SAIB depots. The addition of sucrose acetate isobutyrate (SAIB) to monodisperse Ng-microspheres did not cause a change in the chemical structure. The performances of the microspheres in osteoblast-microsphere interactions were better when the naringin content was 4% than when it was at 2% and 6%. On the first day following the loading of Ng-microspheres (2%, 4%, and 6%) into SAIB depots, the burst release was reduced dramatically from 70.9% to 6.3%, 73.1% to 7.2%, and 73.9% to 9.9%, respectively. In addition, after 8 weeks, the new bone formation rate in the calvarial defects of SD rats receiving Ng-m-SAIB was 53.1% compared to 21.2% for the control group and 16.1% for the microsphere-SAIB group. These results demonstrated that Ng-m-SAIB hybrid depots may have promise in bone regeneration applications.

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“…Lin et al. (2015) demonstrated that combining PLGA microspheres with SAIB depots could reduce the burst release of risperidone to 0.64% after 1 day.…”

Section: Introductionmentioning

confidence: 99%

Electrosprayed naringin-loaded microsphere/SAIB hybrid depots enhance bone formation in a mouse calvarial defect model

et al. 2019

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“…No obvious burst release was observed in formulations S1, S2, and S4 (cumulative release of RM was only 5% in the first 24 h), indicating that drug escape was effectively prevented by the dual-controlled system combining in situ gel with RM-MS. During the formation of the semisolid implant, drug release was strongly inhibited by the controlled release effect of the PLGA MS, which contributed to a low drug diffusion rate from MS into the in-situ gel. Only a small amount of drug derived from the MS surface would be released into the medium during this lag time (Lin et al., 2015 ). Formulations S3 and S5 had a low burst release (13% and 24%, respectively), while formulation S6 exhibited a high initial burst (48%).…”

Section: Resultsmentioning

confidence: 99%

“…Lin et al. ( 2015 ) developed a uniform ultra-small microsphere/sucrose acetate isobutyrate (SAIB) hybrid depot to provide a long-term sustained release system for the water-insoluble drug, Risperidone; it not only reduced the burst release of the SAIB depot, but also eliminated the lag-time of the PLGA microspheres. It is worth considering that most existing clinical medications are hydrophilic small-molecule compounds, and compared to that of water-insoluble drugs, the quick and unstable drug release profiles make it tougher for controlled release of water-soluble drugs.…”

Section: Introductionmentioning

confidence: 99%

Preparation and evaluation of injectable Rasagiline mesylate dual-controlled drug delivery system for the treatment of Parkinson’s disease

Jiang

Zhang

et al. 2017

Drug Delivery

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A microsphere–gel in situ forming implant (MS–Gel ISFI) dual-controlled drug delivery system was applied to a high water-soluble small-molecule compound Rasagiline mesylate (RM) for effective treatment of Parkinson’s disease. This injectable complex depot system combined an in situ phase transition gel with high drug-loading and encapsulation efficiency RM–MS prepared by a modified emulsion-phase separation method and optimized by Box–Behnken design. It was evaluated for in vitro drug release, in vivo pharmacokinetics, and in vivo pharmacodynamics. We found that the RM-MS-Gel ISFI system showed no initial burst release and had a long period of in vitro drug release (60 days). An in vivo pharmacokinetic study indicated a significant reduction (p < .01) in the initial high plasma drug concentration of the RM–MS–Gel ISFI system compared to that of the single RM–MS and RM–in situ gel systems after intramuscular injection to rats. A pharmacodynamic study demonstrated a significant reduction (p < .05) in 6-hydroxydopamine-induced contralateral rotation behavior and an effective improvement (p < .05) in dopamine levels in the striatum of the lesioned side after 28 days in animals treated with the RM–MS–Gel ISFI compared with that of animals treated with saline. MS-embedded in situ phase transition gel is superior for use as a biodegradable and injectable sustained drug delivery system with a low initial burst and long period of drug release for highly hydrophilic small molecule drugs.

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“…The suspensions are known to cause slower absorption than solutions and result in a zero order drug absorption profile (35). In addition, as the time elapsed, the biodegradation of sucrose acetate isobutyrate must also have begun and after four days of administration would slowly have started contributing to the enhancement in drug release from gel depot matrix (36).…”

Section: Discussionmentioning

confidence: 99%

Formulation and in Vivo Pharmacokinetic Studies of Iloperidone Depot Injection

Dubey¹,

Saini²

2019

Acta Poloniae Pharmaceutica - Drug Research

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A Uniform Ultra-Small Microsphere/SAIB Hybrid Depot with Low Burst Release for Long-Term Continuous Drug Release

Abstract: These results demonstrate the potential application of a uniform ultra-small microsphere/SAIB hybrid depot for continuously delivering small drug molecules for long periods of time without burst release.

Cited by 16 publications

References 40 publications

Electrosprayed naringin-loaded microsphere/SAIB hybrid depots enhance bone formation in a mouse calvarial defect model

Electrosprayed naringin-loaded microsphere/SAIB hybrid depots enhance bone formation in a mouse calvarial defect model

Preparation and evaluation of injectable Rasagiline mesylate dual-controlled drug delivery system for the treatment of Parkinson’s disease

Formulation and in Vivo Pharmacokinetic Studies of Iloperidone Depot Injection

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