In Vitro Performance of Carbamazepine Loaded to Various Molecular Weights of Poly (D, L-Lactide-Co-Glycolide)

Barakat, Nahla S.; Radwan, Mahasen A.

doi:10.1080/10717540500308992

Cited by 15 publications

(4 citation statements)

References 31 publications

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“…The absorption band at 1384 cm-1 is due to NH2 rocking. The existence of NH valence vibration at 3462cm −1 is considered as an evidence that CBZ could be neither polymorph II (3474 cm −1 ) nor polymorph I (3484 cm −1 ) [18,25]. This suggests that the tested CBZ is in form of polymorph III.…”

Section: Ftir Studiesmentioning

confidence: 99%

Microsponges for controlled release and enhanced oral bioavailability of carbamazepine

Abdalla

Osman

Nouh

et al. 2021

Journal of Drug Delivery Science and Technology

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The oral absorption and hence the oral bioavailability of carbamazepine (CBZ) is variable even after administration of rapidly dissolving formulation. This problem was attributed to supersaturation of CBZ and transformation to the less soluble carbamazepine dihydrate (CBD). Accordingly, formulation of sustained release products of CBZ is a promising approach to overcome this problem. Microsponges is an emerging formulation which can help in this direction. The aim of this work was to optimize the composition of microsponges for better encapsulation and sustained release of CBZ for oral administration. CBZ microsponges were prepared using quasi emulsion solvent diffusion technique with varying composition of ethyl cellulose and polyvinyl alcohol (PVA). Microsponges were evaluated using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and X-ray diffraction. Production yield, entrapment e ciency and surface morphology of microsponges were assessed in addition to drug release. Optimum formulation was administered orally to albino rabbits to evaluate the oral bioavailability with reference to unprocessed CBZ. The Instrumental analysis re ected the encapsulation of CBZ in amorphous or molecularly dispersed form in the microsponges. The size and entrapment e ciency of the microsponges increased with increasing polymer contents. This was associated with reduction in CBZ release. Optimum formulation enhanced the oral absorption of CBZ. This was manifested by 2.6-fold increase in the area under the plasma concentration versus time curve compared to that of unprocessed CBZ. The study introduced microsponges as promising carriers for sustained oral delivery of CBZ.

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Section: Ftir Studiesmentioning

confidence: 99%

Microsponges for controlled release and enhanced oral bioavailability of carbamazepine

Abdalla

Osman

Nouh

et al. 2021

Journal of Drug Delivery Science and Technology

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“…The results of this study demonstrate that lower initial drug loadings lead to more controlled patterns of drug release, irrespective of the polymer's glycolide content or physical structure. Formulations with theoretical drug loadings of =10% had the smallest initial bursts and thereafter demonstrated gradual, continuous release of LEV, consistent with the published literature 10–12. We hypothesize that at high drug loadings, there is unlikely to be sufficient polymer present to completely entrap the entire drug load within the polymer matrix, leading to unregulated drug release as soon as the material is immersed in fluid.…”

Section: Discussionmentioning

confidence: 99%

“…Formulations with theoretical drug loadings of =10% had the smallest initial bursts and thereafter demonstrated gradual, continuous release of LEV, consistent with the published literature. [10][11][12] We hypothesize that at high drug loadings, there is unlikely to be sufficient polymer present to completely entrap the entire drug load within the polymer matrix, leading to unregulated drug release as soon as the material is immersed in fluid. In contrast, at low drug loadings, the polymer entirely and homogeneously encapsulates the drug such that drug release is primarily dictated by polymer degradation.…”

Section: Discussionmentioning

confidence: 99%

In vivo biocompatibility and in vitro characterization of poly‐lactide‐co‐glycolide structures containing levetiracetam, for the treatment of epilepsy

Halliday

Campbell

Razal

et al. 2011

J Biomedical Materials Res

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Epilepsy is a chronic neurological disorder characterized by recurrent seizures, and is highly resistant to medication with up to 40% of patients continuing to experience seizures whilst taking oral antiepileptic drugs. Recent research suggests that this may be due to abnormalities in the blood-brain barrier, which prevent the passage of therapeutic substances into the brain. We sought to develop a drug delivery material that could be implanted within the brain at the origin of the seizures to release antiepileptic drugs locally and avoid the blood brain barrier. We produced poly-lactide-co-glycolide drop-cast films and wet-spun fibers loaded with the novel antiepileptic drug Levetiracetam, and investigated their morphology, in vitro drug release characteristics, and brain biocompatibility in adult rats. The best performing structures released Levetiracetam constantly for at least 5 months in vitro, and were found to be highly brain biocompatible following month-long implantations in the motor cortex of adult rats. These results demonstrate the potential of polymer-based drug delivery devices in the treatment of epilepsy and warrant their investigation in animal models of focal epilepsy.

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“…PCL je biodegradabilan polimer koji sporo hidrolitički degradira, pa se može smatrati da ne dolazi do značajnije degradacije polimerne matrice za vreme trajanja eksperimenta kontrolisanog otpuštanja od 72 h, odnosno može se zanemariti otpuštanje leka uzrokovano degradacijom mikrosfera. Kinetika otpuštanja leka je ispitana na svim uzorcima korišćenjem različitih matematičkih modela otpuštanja leka: kinetika nultog reda (jednačina (1)), kao i Higuchi (jednačina (2)) i Peppas-ov model (jednačina ( 3)) [28][29][30]:…”

Section: Kinetika Otpuštanja Lekaunclassified

Optimization of preparation conditions of poly(ε-caprolactone) microspheres for controlled release of carbamazepine

Pepic¹,

Andjelkovic²,

Nikolić³

et al. 2010

Hem Ind

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Poly (?-caprolactone), PCL, is an aliphatic polyester suitable for controlled drug release due to its biodegradability, biocompatibility, non-toxicity and high permeability to many therapeutic drugs. This study investigates the effect of the preparation parameters on the size and the morphology of the PCL microspheres and on the release profile of carbamazepine from these microspheres. The PCL microspheres were prepared using oil-in-water (o/w) emulsion solvent evaporation method with the poly(vinyl alcohol), PVA, as the emulsion stabilizer. The influence of the stirring rate applied during the emulsion formation, the homogenization time and the emulsifier concentration on diameter and size distribution of the microspheres was analyzed by scanning electron microscope (SEM). The initial emulsion was formed applying high stirring rates of 10000, 18000 and 23000 rpm, for homogenization times: 5, 10 and 15 min. The diameter was strongly influenced by the stirring rate, and the average particle size decreased from 9.2 to 2.8 ?m with the increase of the stirring rate. Increasing the amount of PVA in the water phase from 0.2 to 1 mass% improved stabilization of the oil droplets and led to a slight decrease of the average particle diameter. Drug-loaded microspheres were prepared by the same technique using different amounts of carbamazepine (10 and 15 mass%), under given conditions (1 mass% PVA, stirring rate of 18000 rpm for a period of 5 min of emulsion formation). Additionally, microspheres were prepared by applying low stirring rate of 1000 rpm with 10 and 15 mass% of the drug. The SEM analysis showed that microspheres created with 18000 rpm stirring rate, had average diameters of 3-4 ?m, and the microspheres prepared with 1000 rpm stirring rate were larger than 100 ?m. It was also observed that, in the case of the large microspheres, carbamazepine was deposited on their surfaces, while the small microspheres had smooth surfaces without observable drug crystals. The encapsulation efficiency and the release behavior of the carbamazepine were examined using high performance liquid chromatography-ultraviolet spectroscopy (HPLC-UV). The drug encapsulation efficiencies were in the range from 69 to 81%, and were increasing with the increase of the amount of carbamazepine in both series. In vitro release experiments were carried out in the phosphate buffer solution (pH 7) at 37?C. The release rate was influenced by the microspheres size and morphology. The larger microspheres released more carbamazepine (85-95%) compared to the small ones (50-65%) for the same period. This behavior was attributed to the different drug distribution in the PCL matrix. Different mathematical models were used to describe drug release kinetics. It was concluded that the mechanism of the carbamazepine release from the microspheres was diffusion-controlled, independent on the type of microspheres. The kinetic parameters showed that the release of carbamazepine was slower from the smaller microspheres, probably as a result of more even distribution of the drug in the polymer matrix.

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In Vitro Performance of Carbamazepine Loaded to Various Molecular Weights of Poly (D, L-Lactide-Co-Glycolide)

Cited by 15 publications

References 31 publications

Microsponges for controlled release and enhanced oral bioavailability of carbamazepine

Microsponges for controlled release and enhanced oral bioavailability of carbamazepine

In vivo biocompatibility and in vitro characterization of poly‐lactide‐co‐glycolide structures containing levetiracetam, for the treatment of epilepsy

Optimization of preparation conditions of poly(ε-caprolactone) microspheres for controlled release of carbamazepine

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