Dissolution and Permeation Properties of Naproxen From Solid-State Systems With Chitosan

Corti, Giovanna; Maestrelli, Francesca; Cirri, Marzia; Mura, Paola; Zerrouk, Naïma

doi:10.1080/10717540802006955

Cited by 19 publications

(9 citation statements)

References 22 publications

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“…[50][51][52] The results show the absence of any interaction between the drug and stabilizer PVA ( Figure 6). …”

mentioning

confidence: 85%

A top-down technique to improve the solubility and bioavailability of aceclofenac: in vitro and in vivo studies

Narayan¹,

Pednekar²,

Bhuyan³

et al. 2017

IJN

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The aim of the present work was to tackle the solubility issue of a biopharmaceutics classification system (BCS)-II drug, aceclofenac. Although a number of attempts to increase the aqueous solubility have been made, none of the methods were taken up for scale-up. Hence size reduction technique by a top-down approach using wet milling process was utilized to improve the solubility and, consequently, the dissolution velocity of aceclofenac. The quality of the final product was ensured by Quality by Design approach wherein the effects of critical material attributes and critical process parameters were assessed on the critical quality attributes (CQAs) of nanocrystals. Box–Behnken design was applied to evaluate these effects on critical quality attributes. The optimized nanocrystals had a particle size of 484.7±54.12 nm with a polydispersity index (PDI) of 0.108±0.009. The solid state characterization of the formulation revealed that the crystalline nature of the drug was slightly reduced after the milling process. With the reduced particle size, the solubility of the nanocrystals was found to increase in both water and 0.1 N HCl when compared with that of unmilled pure aceclofenac. These results were further supported by in vitro release studies of nanocrystals where an appreciable dissolution velocity with 100.07%±2.38% release was observed for aceclofenac nanocrystals compared with 47.66%±4.53% release for pure unmilled aceclofenac at the end of 2 h. The in vivo pharmacokinetic data generated showed a statistically significant increase in the C max for aceclofenac nanocrystals of 3.75±0.28 µg/mL (for pure unmilled aceclofenac C max was 1.96±0.17 µg/mL). The results obtained indicated that the developed nanocrystals of aceclofenac were successful in improving the solubility, thus the absorption and bioavailability of the drug. Hence, it may be a viable and cost-effective alternative to the current therapy.

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“…[50][51][52] The results show the absence of any interaction between the drug and stabilizer PVA ( Figure 6). …”

mentioning

confidence: 85%

A top-down technique to improve the solubility and bioavailability of aceclofenac: in vitro and in vivo studies

Narayan¹,

Pednekar²,

Bhuyan³

et al. 2017

IJN

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“…CH has been shown to improve the dissolution rate of poorly soluble drugs and thus can be exploited for bioavailability enhancement of such drugs 1 ; the phenomenon of enhanced dissolution can be related to decrease drug crystallinity and size and the polymer wetting effect. 2,3 There are numbers of CH salts (such as CH hydrochloride, 3,4 glutamate, 3,4 and ascorbate 5 ) and derivatives (e.g., N-carboxymethylchitosan, 6 N-trimethylchitosan, [7][8][9] and methylpyrrolidinone CH 10 ), which have better characteristics such as solubility, mucoadhesiveness, and penetration enhancement ability compared with CH itself.…”

Section: Introductionmentioning

confidence: 99%

Influence of Chitosan Glutamate on the in vivo Intranasal Absorption of Rokitamycin from Microspheres

Gavini

Rassu

Ferraro

et al. 2011

Journal of Pharmaceutical Sciences

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“…Moreover, CS exhibits several attractive biological properties, such as nontoxicity, good biocompatibility and biodegradability, wide availability in nature, and low cost (13). Some researches have been reported that CS as carrier increased the dissolution properties and bioavailability of insoluble drugs (14)(15)(16)(17)(18)(19)(20). Taking all into account, CS was chosen as a desirable carrier to disperse TEL in SD systems.…”

Section: Introductionmentioning

confidence: 99%

Dissolution Properties and Physical Characterization of Telmisartan–Chitosan Solid Dispersions Prepared by Mechanochemical Activation

et al. 2013

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Abstract. Solid dispersion systems of telmisartan (a poorly water-soluble antihypertension drug) with biopolymer carrier chitosan have been investigated in this study. The mechanism of solubilization of chitosan for drug has been studied. In addition, the influence of several factors was carefully examined, including the preparation methods, the drug/carrier weight ratios, and the milling time. Drug dissolution and physical characterization of different binary systems were studied by in vitro dissolution test, particle size distribution, Fourier transform infrared spectroscopy, differential scanning calorimetry, powder X-ray diffractometry, and scanning electron microscopy. The results presented that the weak basic property of chitosan appeared as the main driving force for the drug dissolution enhancement. Other effects such as decreased drug crystallinity and size played a positive contributory role. Among the preparation methods, cogrinding was the best method showing strong drug amorphization, reduced particle size, and enhanced dissolution. The drug dissolution markedly improved with increasing the amount of chitosan in solid mixtures. As a result, a significant effect of chitosan increasing telmisartan dissolution has been demonstrated, and cogrinding in a roll ball mill was the best way to prepare solid dispersions, which had high degree of uniformity in drug content and had a practical application in manufacturing.

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Dissolution and Permeation Properties of Naproxen From Solid-State Systems With Chitosan

Cited by 19 publications

References 22 publications

A top-down technique to improve the solubility and bioavailability of aceclofenac: in vitro and in vivo studies

A top-down technique to improve the solubility and bioavailability of aceclofenac: in vitro and in vivo studies

Influence of Chitosan Glutamate on the in vivo Intranasal Absorption of Rokitamycin from Microspheres

Dissolution Properties and Physical Characterization of Telmisartan–Chitosan Solid Dispersions Prepared by Mechanochemical Activation

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