Improved physical stability and injectability of non-aqueous in situ PLGA microparticle forming emulsions

Voigt, M.; Koerber, Martin; Bodmeier, Roland

doi:10.1016/j.ijpharm.2012.05.029

Cited by 25 publications

(13 citation statements)

References 28 publications

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“…The injection force is divided into three parts: (a) overcoming the resistance force of the syringe plunger; (b) imparting kinetic energy to the liquid; and (c) forcing the liquid through the needle (Allahham et al., 2004 ). The main parameters of syringeability studies are plunger-stopper breakloose force (PBF), maximum force and dynamic glide force (DGF) (Voigt et al., 2012 ). PBF refers to the force required to initiate the movement of the plunger; maximum force ( F max ): the highest force measured during the course of injection which was always equal to the PBF; DGF was referred to the force required to sustain the movement of the plunger.…”

Section: Resultsmentioning

confidence: 99%

“…In order to ensure the syringeability will meet the requirement which the upper limit of injection force was set at 10 N and which is the lower the better in treatment process (Cilurzo et al., 2011 ; Voigt et al., 2012 ), the concentration of copolymer solution should be as low as possible. After contract the variation trend of gelation temperature and required force of copolymer solutions on different concentration ( Figure 2(f) ), the result shows that the variation trend was reversed with concentration increase.…”

Section: Resultsmentioning

confidence: 99%

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Synthesis, physicochemical properties and ocular pharmacokinetics of thermosensitive in situ hydrogels for ganciclovir in cytomegalovirus retinitis treatment

Wang

Sun

et al. 2017

Drug Delivery

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Ganciclovir (GCV) is one of the most widely used antiviral drugs for the treatment of cytomegalovirus (CMV) retinitis. In this context, the aim of this study was to design in situ thermosensitive hydrogels for GCV ocular delivery by intravitreal injection to achieve sustained drug release behavior and improved ocular bioavailability in the treatment of CMV retinitis. A thermosensitive poly-(β-butyrolactone-co-lactic acid)-polyethylene glycol-poly (β-butyrolactone-co-lactic acid) (PBLA-PEG-PBLA) triblock copolymer was synthesized by ring-opening polymerization and characterization. The GCV-loaded PBLA-PEG-PBLA in situ hydrogels (15%, w/w) were then prepared with drug concentration at 2 mg·mL−1 and the gelation temperatures, rheological properties, in vitro degradation and syringeability of in situ hydrogels for intravitreal injection were also investigated. Membraneless dissolution model was used to explore drug release behavior of PBLA-PEG-PBLA in situ hydrogel. The results indicated that more than 45 and 85% of GCV can be released within 24 and 96 h, respectively, which was verified by a non-Fickian diffusion mechanism. In vivo ocular pharmacokinetics study showed that area under drug-time curve (AUC) and half-life of PBLA-PEG-PBLA in situ hydrogel was higher (AUC was 61.80 μg·mL−1·h (p < .01) and t 1/2 was 10.29 h in aqueous humor; AUC was 1008.66 μg·mL−1·h (p < .01) and t 1/2 was 13.26 h (p < .01) in vitreous) than GCV injection with extended therapeutic activity. Based on obtained results, it was concluded that the thermosenstive PBLA-PEG-PBLA in situ hydrogel is a promising carrier of GCV for intravitreal injection.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Synthesis, physicochemical properties and ocular pharmacokinetics of thermosensitive in situ hydrogels for ganciclovir in cytomegalovirus retinitis treatment

Wang

Sun

et al. 2017

Drug Delivery

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“…Consequently, it is less painful and higher polymer concen- cence of emulsion droplets could occur during their solidification [60].…”

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confidence: 99%

PLGA in situ implants formed by phase inversion: Critical physicochemical parameters to modulate drug release

Parent

Nouvel²,

Koerber³

et al. 2013

Journal of Controlled Release

207

172

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“…[6] Such systems which can replace conventional emulsions where the presence of water to be avoided. [7][8][9][10][11][12][13][14] Such systems can reduce the inherent limitations and facilitates the formation of solubilized phases from which absorption may occur. Unfortunately, the major difficulty in formulating NANE arises from the lack of appropriate data on surfactant action in relevant non-aqueous media, or indeed, the dearth of suitable surfactant designed for such specialized system.…”

Section: Introductionmentioning

confidence: 99%

Untitled

Payghan

2016

AJP

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Aim: The study was to design a stable non-aqueous nanoemulsion (NANE) using cosmetically approved ingredients as a vehicle for the water sensitive active ingredients. Materials and Methods: NANE was designed to increase the dermal penetration and permeation and study solubility and dermal bioavailability of cholecalciferol. For better compliance incorporated the NANEs in cosmetics or personal care products. A non-aqueous system was obtained with glycerin and mineral oil stabilized by glycerol monosterate. It was observed that emulsification behavior is completely unpredictable and conventional theories of emulsification and HLB system cannot be applied here. An optimized non-aqueous cream was obtained through implementation of Box-Behnken experimental design. Cholecalciferol was used as model drug which converts into dehydro cholecalciferol in the presence of water. Result and Discussion: NANE was evaluated by pH, rheology, spreadability, drug content, globule size analysis, zeta potential, and stability. The stability studies (agitation, centrifugation, freeze thaw cycle, accelerated stability) were carried out at 5°C, 25°C and 40°C. Cream was stable at 5°C and 25°C. In vitro drug release shows slow permeation rate but increased retention of cholecalciferol in skin. A comparative study with aqueous formulation shows that non-aqueous cream offers a good stability for cholecalciferol. Conclusion: Results proved that NANE can be used as vehicle for the poorly water-soluble drug, suspension vehicles, and oleogels.

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Improved physical stability and injectability of non-aqueous in situ PLGA microparticle forming emulsions

Cited by 25 publications

References 28 publications

Synthesis, physicochemical properties and ocular pharmacokinetics of thermosensitive in situ hydrogels for ganciclovir in cytomegalovirus retinitis treatment

Synthesis, physicochemical properties and ocular pharmacokinetics of thermosensitive in situ hydrogels for ganciclovir in cytomegalovirus retinitis treatment

PLGA in situ implants formed by phase inversion: Critical physicochemical parameters to modulate drug release

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