Design of controlled release inert matrices of naltrexone hydrochloride based on percolation concepts

Caraballo, Isidoro; Melgoza, Luz María; Álvarez-Fuentes, Josefa; Soriano, Mabel; Rabasco, A. M.

doi:10.1016/s0378-5173(98)00415-3

Cited by 32 publications

(12 citation statements)

References 14 publications

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“…Because of the poor compliance of the addicted patients that regularly use naltrexone hydrochloride, the development of novel extended-release systems that can provide an effective drug concentration in the blood for a long time after just one injection is desirable [16][17][18].…”

Section: Introductionmentioning

confidence: 99%

Preparation and analysis of a sustained drug delivery system by PLGA–PEG–PLGA triblock copolymers

et al. 2012

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Traditional drug delivery systems that are based on multiple dosing are usually accompanied by many shortcomings, including unwanted fluctuations in the plasma concentration of the drug and poor patient compliance. In this study, we aimed to synthesize a polymeric drug delivery system based on a triblock copolymer of PLGA-PEG1000-PLGA and investigate its application as a controlled drug delivery system. Naltrexone hydrochloride and vitamin B12 were used as model drugs here. The copolymer was successfully synthesized by the ring-opening method. A phase transition analysis indicated that the copolymer is in gel at body temperature. The release profiles from the formulations showed a higher initial release followed by a slower pattern for up to 4 weeks. More than 50 % of the vitamin B12 and 60 % of the naltrexone hydrochloride were released during this period.

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Section: Introductionmentioning

confidence: 99%

Preparation and analysis of a sustained drug delivery system by PLGA–PEG–PLGA triblock copolymers

et al. 2012

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“…Early trials have suggested that the sustained release of naltrexone may be appropriate for the management of either alcohol or opioid dependence (5,13,14). There are several systems for the subcutaneous implantation of naltrexone hydrochloride (9,(15)(16)(17), but this route of administration requires intricate technology, and it is too expensive (8).…”

Section: Introductionmentioning

confidence: 99%

“…Naltrexone was the first drug to receive FDA approval to treat alcohol dependence (4)(5)(6)(7). Because of the extensive first-pass metabolism in the liver, only 5-20 % of the oral dosage of this drug reaches the systemic circulation unchanged (4,8). In addition, there are certain side effects associated with its oral administration, such as abdominal pain, nausea, and vomiting (9).…”

Section: Introductionmentioning

confidence: 99%

Preparation and Investigation of Sustained Drug Delivery Systems Using an Injectable, Thermosensitive, In Situ Forming Hydrogel Composed of PLGA–PEG–PLGA

et al. 2012

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Abstract. In situ gelling systems are very attractive for pharmaceutical applications due to their biodegradability and simple manufacturing processes. The synthesis and characterization of thermosensitive poly(D,L-lactic-co-glycolic acid) (PLGA)-polyethylene glycol (PEG)-PLGA triblock copolymers as in situ gelling matrices were investigated in this study as a drug delivery system. Ring-opening polymerization using microwave irradiation was utilized as a novel technique, and the results were compared with those using a conventional method of polymerization. The phase transition temperature and the critical micelle concentration (CMC) of the copolymer solutions were determined by differential scanning calorimetry and spectrophotometry, respectively. The size of the micelles was determined with a light scattering method. In vitro drug release studies were carried out using naltrexone hydrochloride and vitamin B12 as model drugs. The rate and yield of the copolymerization process via microwave irradiation were higher than those of the conventional method. The copolymer structure and concentration played critical roles in controlling the sol-gel transition temperature, the CMC, and the size of the nanomicelles in the copolymer solutions. The rate of drug release could be modulated by the molecular weight of the drugs, the concentration of the copolymers, and their structures in the formulations. The amount of release versus time followed zero-order release kinetics for vitamin B12 over 25 days, in contrast to the Higuchi modeling for naltrexone hydrochloride over a period of 17 days. In conclusion, PLGA-PEG1500-PLGA with a lactide-to-glycolide ratio of 5:1 is an ideal system for the long-acting, controlled release of naltrexone hydrochloride and vitamin B12.

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“…The more complex the microstructure of a system, the lower the percolation threshold [Eq. (14)]. The inherently complex nature of the underlying microstructure of the benzoic acid/poly(vinyl stearate) system therefore results in a naturally low percolation threshold which is also influenced by the volume fraction of the non-classically percolating regions of the polymer.…”

Section: The Porous Microstructurementioning

confidence: 99%

Percolative Transport and Cluster Diffusion Near and Below the Percolation Threshold of a Porous Polymeric Matrix

Hastedt¹,

Wright

2006

Pharm Res

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A model describing transport near and below the percolation threshold in matrices composed of two phases, polymer and drug, was developed. The percolation model developed accounts for diffusion within the porous structure and through the inert, insoluble polymeric amorphous regions of the matrix. The low percolation threshold and subsequently high coordination was concluded to be due to the biphasic classical porous and nonclassical polymeric diffusional transport mechanisms associated with the system studied.

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Design of controlled release inert matrices of naltrexone hydrochloride based on percolation concepts

Cited by 32 publications

References 14 publications

Preparation and analysis of a sustained drug delivery system by PLGA–PEG–PLGA triblock copolymers

Preparation and analysis of a sustained drug delivery system by PLGA–PEG–PLGA triblock copolymers

Preparation and Investigation of Sustained Drug Delivery Systems Using an Injectable, Thermosensitive, In Situ Forming Hydrogel Composed of PLGA–PEG–PLGA

Percolative Transport and Cluster Diffusion Near and Below the Percolation Threshold of a Porous Polymeric Matrix

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