Physicochemical aspects of drug release. VIII. The relation between particle size and surface specific dissolution rate in agitated suspensions

Bisrat, Mikael; Nyström, Christer

doi:10.1016/0378-5173(88)90235-9

Cited by 110 publications

(48 citation statements)

References 15 publications

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“…Breviscapine release from the Bre-NLC occurred in a very slow manner with a cumulative release of ~50% over 48 h. The Hixson-Crowel model matched the release style (R 2 =0.9795) well. The Hixson-Crowell cube root law indicated that the drug was released from the system by progressive dissolution, in which there is a change in the surface area and diameter of the particles [37][38][39] . It was proven that the mechanism of breviscapine release from the NLC was controlled by an erosion process.…”

Section: Discussionmentioning

confidence: 99%

Development of ionic-complex-based nanostructured lipid carriers to improve the pharmacokinetic profiles of breviscapine

Zheng

Shan

et al. 2013

Acta Pharmacol Sin

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Aim: Breviscapine isolated from the Chinese herb Erigeron breviscapus (Vant) Hand-Mazz is widely used to treat cardiovascular and cerebrovascular diseases. The aim of this study was to improve the pharmacokinetic profiles of breviscapine using nanostructured lipid carrier based on an ionic complex formation. Methods: Breviscapine nanostructured lipid carrier (Bre-NLC) was prepared using the thin film homogenization method. The morphology of Bre-NLCs was determined using transmission electron microscopy. The mean particle size, polydispersity index, zeta-potential analysis and entrapment efficiency were analized. In vitro release was studied using the dialysis method. In vitro stability was studied in fresh plasma and liver slurry of rats. In vivo pharmacokinetics was analyzed in rats after intravenous injection of a dose equivalent to breviscapine (10 mg/kg). Results: The Bre-NLCs were spherical with a mean particle size of ~170 nm, a zeta potential of ~20 mV and a high entrapment efficiency of ~89%. Compared with a commercially available solution, a substantial decrease in the cumulative release of breviscapine was found for the Bre-NLCs. The NLC has a significantly protective effect against the liver enzyme degradation of breviscapine. After intravenous administration in rats, the Bre-NLCs exhibited a 32 times increase in the AUC 0-t and a 12 times increase in T 1/2 as compared to the commercially available breviscapine solution. Conclusion:The results demonstrate that the NLC has great potential to use as a novel sustained release system for breviscapine.

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Section: Discussionmentioning

confidence: 99%

Development of ionic-complex-based nanostructured lipid carriers to improve the pharmacokinetic profiles of breviscapine

Zheng

Shan

et al. 2013

Acta Pharmacol Sin

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“…This was carried out using USP II dissolution apparatus (Hanson Research Corp., Chatsworth, CA, USA) containing 900 mL Sorenson's phosphate buffer pH 6.8 as dissolution medium at 37°C and stirred at 50 rpm. 37 Dissolution samples were withdrawn at 5,10,15,20,30,45,60, and 90 minutes, with replacement of an equal volume of dissolution medium. The samples were filtered and analyzed using an UV spectrophotometer as mentioned earlier.…”

Section: In Vitro Dissolution Studymentioning

confidence: 99%

“…It is believed that a difference in particle diameter could correspond to a difference in the parameter L. 59 Bisrat and Nyström have shown that, for solids dispersed in a liquid medium under agitation, a decrease in PS probably leads to a decrease in both L and V. 60 The net effect is reduced h H . 61 This decrease in diffusional thickness h leads to an increase in the concentration gradient (Cs-Ct)/h, which consequently increases the dissolution rate.…”

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confidence: 99%

Preparation, optimization, and in vitro simulated inhalation delivery of carvedilol nanoparticles loaded on a coarse carrier intended for pulmonary administration

Abdelbary¹,

Al-mahallawi²,

Abdelrahim³

et al. 2015

IJN

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Carvedilol (CAR) is a potent antihypertensive drug but has poor oral bioavailability (24%). A nanosuspension suitable for pulmonary delivery to enhance bioavailability and bypass first-pass metabolism of CAR could be advantageous. Accordingly, the aim of this work was to prepare CAR nanosuspensions and to use artificial neural networks associated with genetic algorithm to model and optimize the formulations. The optimized nanosuspension was lyophilized to obtain dry powder suitable for inhalation. However, respirable particles must have a diameter of 1–5 µm in order to deposit in the lungs. Hence, mannitol was used during lyophilization for cryoprotection and to act as a coarse carrier for nanoparticles in order to deliver them into their desired destination. The bottom-up technique was adopted for nanosuspension formulation using Pluronic stabilizers (F127, F68, and P123) combined with sodium deoxycholate at 1:1 weight ratio, at three levels with two drug loads and two aqueous to organic phase volume ratios. The drug crystallinity was studied using differential scanning calorimetry and powder X-ray diffractometry. The in vitro emitted doses of CAR were evaluated using a dry powder inhaler sampling apparatus and the aerodynamic characteristics were evaluated using an Andersen MKII cascade impactor. The artificial neural networks results showed that Pluronic F127 was the optimum stabilizer based on the desired particle size, polydispersity index, and zeta potential. Results of differential scanning calorimetry combined with powder X-ray diffractometry showed that CAR crystallinity was observed in the lyophilized nanosuspension. The aerodynamic characteristics of the optimized lyophilized nanosuspension demonstrated significantly higher percentage of total emitted dose (89.70%) and smaller mass median aerodynamic diameter (2.80 µm) compared with coarse drug powder (73.60% and 4.20 µm, respectively). In summary, the above strategy confirmed the applicability of formulating CAR in the form of nanoparticles loaded on a coarse carrier suitable for inhalation delivery.

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“…It is believed that a difference in particle diameter could correspond to a difference in the parameter L. 51 Bisrat and Nyström have shown that, for solids dispersed in a liquid medium under agitation, a decrease in PS probably leads to a decrease in both L and V. 52 The net effect is reduced h H . 53 This decrease in diffusional thickness h leads to an increase in the concentration gradient (Cs-Ct)/h, which consequently increases the dissolution rate.…”

Section: In Vitro Dissolution Studymentioning

confidence: 99%

Nanosizing of a poorly soluble drug: technique optimization, factorial analysis, and pharmacokinetic study in healthy human volunteers

Elsayed¹,

Abdelbary²,

Elshafeey³

2014

IJN

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Context Diacerein (DCN) has low aqueous solubility (3.197 mg/L) and, consequently, low oral bioavailability (35%–56%). To increase both the solubility and dissolution rate of DCN while maintaining its crystalline nature, high pressure homogenization was used but with only a few homogenization cycles preceded by a simple bottom-up technique. Methods The nanosuspensions of DCN were prepared using a combined bottom-up/top-down technique. Different surfactants – polyvinyl alcohol, sodium deoxycholate, and sodium dodecyl sulfate – with different concentrations were used for the stabilization of the nanosuspensions. Full factorial experimental design was employed to investigate the influence of formulation variables on nanosuspension characteristics using Design-Expert ® Software. Particle size (PS), zeta potential, saturation solubility, in vitro dissolution, and drug crystallinity were studied. Moreover, the in vivo performance of the optimized formula was assessed by bioavailability determination in healthy human volunteers. Results The concentration of surfactant had a significant effect on both the PS and polydispersity index values. The 1% surfactant concentration showed the lowest PS and polydispersity index values compared with other concentrations. Both type and concentration of surfactant had significant effects on the zeta potential. Formula F8 (containing 1% sodium deoxycholate) and Formula F12 (containing 1% sodium dodecyl sulfate) had the highest desirability values (0.952 and 0.927, respectively). Hence, they were selected for further characterization. The saturated solubility and mean dissolution time, in the case of F8 and F12, were significantly higher than the coarse drug powder. Techniques utilized in the nanocrystals’ preparation had no effect on DCN crystalline state. The selected formula (F12) showed a higher bioavailability compared to the reference market product with relative bioavailability of 131.4%. Conclusion The saturation solubility, in vitro dissolution rate and relative bioavailability of DCN were significantly increased after nanocrystallization. Less time and power consumption were applied by the combination of bottom-up and top-down techniques.

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Physicochemical aspects of drug release. VIII. The relation between particle size and surface specific dissolution rate in agitated suspensions

Cited by 110 publications

References 15 publications

Development of ionic-complex-based nanostructured lipid carriers to improve the pharmacokinetic profiles of breviscapine

Development of ionic-complex-based nanostructured lipid carriers to improve the pharmacokinetic profiles of breviscapine

Preparation, optimization, and in vitro simulated inhalation delivery of carvedilol nanoparticles loaded on a coarse carrier intended for pulmonary administration

Nanosizing of a poorly soluble drug: technique optimization, factorial analysis, and pharmacokinetic study in healthy human volunteers

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