An in situ gelling system for parenteral delivery

Haglund, Bert O.; Joshi, Rajashree; Himmelstein, Kenneth J.

doi:10.1016/0168-3659(96)01333-8

Cited by 62 publications

(27 citation statements)

References 7 publications

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“…Thermally induced gelling systems show thermoreversible sol/gel transitions and are characterized by a lower critical solution temperature (22)(23)(24)(25). They are liquid at room temperature and produce a gel at and above the lower critical solution temperature (22)(23)(24)(25). The incorporation of cubosomes into a thermoresponsive gel should increase drug loading while, in all probability, yielding a lower, more prolonged drug release compared with pure gel (26).…”

Section: Introductionmentioning

confidence: 99%

“…Such systems have been suggested for the delivery of cells or biopharmaceuticals that are susceptible to heat or organic solvents (21). Thermally induced gelling systems show thermoreversible sol/gel transitions and are characterized by a lower critical solution temperature (22)(23)(24)(25). They are liquid at room temperature and produce a gel at and above the lower critical solution temperature (22)(23)(24)(25).…”

Section: Introductionmentioning

confidence: 99%

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Nanostructured Cubosomes in a Thermoresponsive Depot System: An Alternative Approach for the Controlled Delivery of Docetaxel

et al. 2015

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Abstract. The aim of the present study was to develop and evaluate a thermoresponsive depot system comprising of docetaxel-loaded cubosomes. The cubosomes were dispersed within a thermoreversible gelling system for controlled drug delivery. The cubosome dispersion was prepared by dilution method, followed by homogenization using glyceryl monooleate, ethanol and Pluronic ® F127 in distilled water. The cubosome dispersion was then incorporated into a gelling system prepared with Pluronic ® F127 and Pluronic ® F68 in various ratios to formulate a thermoresponsive depot system. The thermoresponsive depot formulations undergo a thermoreversible gelation process i.e., they exists as free flowing liquids at room temperature, and transforms into gels at higher temperatures e.g., body temperature, to form a stable depot in aqueous environment. The mean particle size of the cubosomes in the dispersion prepared with Pluronic ® F127, with and without the drug was found to be 170 and 280 nm, respectively. The prepared thermoresponsive depot system was evaluated by assessing various parameters like time for gelation, injectability, gel erosion, and in-vitro drug release. The drug-release studies of the cubosome dispersion before incorporation into the gelling system revealed that a majority (∼97%) of the drug was released within 12 h. This formulation also showed a short lag time (∼3 min). However, when incorporated into a thermoresponsive depot system, the formulation exhibited an initial burst release of ∼21%, and released only ∼39% drug over a period of 12 h, thus indicating its potential as a controlled drug delivery system.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Nanostructured Cubosomes in a Thermoresponsive Depot System: An Alternative Approach for the Controlled Delivery of Docetaxel

et al. 2015

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“…During the last two decades, injectable in situ gels have attracted considerable attention as polymeric drug carriers (Haglund et al, 1996), and then great interest has arisen on the applications of in situ gels in injectable drug delivery systems (Park et al, 2013;Fan et al, 2014;Lopez-Noriega et al, 2014;Ni et al, 2014;Peng et al, 2014). These systems are in situ gel delivery systems, exposed to body temperature ($37 C), are capable of getting converted to a very high viscous gel, though remaining fluid at room temperature (He et al, 2008).…”

Section: Introductionmentioning

confidence: 99%

Bleomycin A6-loaded anionic liposomes with in situ gel as a new antitumoral drug delivery system

Ding

Hou

et al. 2014

Drug Delivery

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The goal is to develop an in situ gel system comprising anionic liposomes (AL) containing bleomycin A6 (BLM A6) dispersed within the thermosensitive in situ gel for sustained release. The results indicated that the gelation temperature decreased due to AL within gel. Similarly, viscosity and mechanical parameters, such as gel strength for gel, could be enhanced by inducing lipid material with negative charge (phosphatidylglycerol) at 37 C, which provided against corrosion at physiological condition. The in vitro release experiments performed with a dialysis method revealed that in situ gel with AL exhibited the longer drug-release period compared to that with or without nonionic liposomes. An in vivo fluorescence imaging study suggested that the gel with AL loading FITC-BLM A6 stayed in administration site at least for five days. A thermosensitive in situ gel with anionic liposome was a promising carrier for hydrophilic BLM A6, to be used in parenteral delivery system for anti-tumor treatment. KeywordsAnionic liposome, bleomycin A6, in situ gel, mechanical parameter, retention in vivo History

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“…Responsive hydrogel networks consisting of polymethacrylic acid (PMAA) and polyethylene glycol (PEG) are classic examples of pH-sensitive carriers that exhibit swelling transitions in response to changes in pH [9,10] . PEG and PMAA may be associated to form 2 hydrogen-bonded complexes under acidic conditions.…”

Section: Introductionmentioning

confidence: 99%

“…The results were compatible with each other. The carboxylic acid content of copolymers was determined according to the method described in the literature [10] . The molecular weight of polymers was measured by gel permeation chromatography (GPC) using a Waters model 150-C (Milford, MA) containing 4 Shodex GPC KF-800 series columns (SDK, Tokyo, Japan).…”

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confidence: 99%

Synthesis and characterization of methacrylic derivatives of 5-amino salicylic acid with pH-sensitive swelling properties

2001

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The purpose of this study is to develop novel colon-specific drug delivery systems with pHsensitive swelling and drug release properties. Methacrylic-type polymeric prodrugs with different content levels of 5-amino salicylic acid (5-ASA) were synthesized by free radical copolymerization of metacrylic acid (MAA), polyethylene glycol monomethacrylate (PEGMA), and a methacrylic derivative of 5 -ASA (methacryloyloxyethyl 5 -amino salicylate [MOES]). The copolymers were characterized, and the drug content of the copolymers was determined. The effect of copolymer composition on the swelling behavior and hydrolytic degradation was studied in simulated gastric fluid (SGF, pH 1.2) and simulated intestinal fluid (SIF, p H 7.2). The swelling and hydrolytic behavior of the copolymers was dependent on the content of MAA groups and caused a decrease in gel swelling in SGF or an increase in gel swelling in SIF. Drug release studies showed that increasing content of MAA in the copolymer enhances the hydrolysis in SIF but has no effect in SGF. The results suggest that hydrogen-bonded complexes are formed between MAA and PEG pendant groups and that these pH-sensitive systems could be useful for preparation of a controlledrelease formulation of 5-ASA.

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An in situ gelling system for parenteral delivery

Cited by 62 publications

References 7 publications

Nanostructured Cubosomes in a Thermoresponsive Depot System: An Alternative Approach for the Controlled Delivery of Docetaxel

Nanostructured Cubosomes in a Thermoresponsive Depot System: An Alternative Approach for the Controlled Delivery of Docetaxel

Bleomycin A6-loaded anionic liposomes with in situ gel as a new antitumoral drug delivery system

Synthesis and characterization of methacrylic derivatives of 5-amino salicylic acid with pH-sensitive swelling properties

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