scholarly journals Modeling the Release Kinetics of Poorly Water-Soluble Drug Molecules from Liposomal Nanocarriers

2011 ◽  
Vol 2011 ◽  
pp. 1-10 ◽  
Author(s):  
Stephan Loew ◽  
Alfred Fahr ◽  
Sylvio May

Liposomes are frequently used as pharmaceutical nanocarriers to deliver poorly water-soluble drugs such as temoporfin, cyclosporine A, amphotericin B, and paclitaxel to their target site. Optimal drug delivery depends on understanding the release kinetics of the drug molecules from the host liposomes during the journey to the target site and at the target site. Transfer of drugs in model systems consisting of donor liposomes and acceptor liposomes is known from experimental work to typically exhibit a first-order kinetics with a simple exponential behavior. In some cases, a fast component in the initial transfer is present, in other cases the transfer is sigmoidal. We present and analyze a theoretical model for the transfer that accounts for two physical mechanisms, collisions between liposomes and diffusion of the drug molecules through the aqueous phase. Starting with the detailed distribution of drug molecules among the individual liposomes, we specify the conditions that lead to an apparent first-order kinetic behavior. We also discuss possible implications on the transfer kinetics of (1) high drug loading of donor liposomes, (2) attractive interactions between drug molecules within the liposomes, and (3) slow transfer of drugs between the inner and outer leaflets of the liposomes.

Materials ◽  
2019 ◽  
Vol 12 (5) ◽  
pp. 730 ◽  
Author(s):  
Anna Lisik ◽  
Witold Musiał

The aim of this study was to verify the effect of the formulation on the release kinetics of active substances from preparations containing iron ions using in-line conductivity measurements. A simple, fast method was developed and may be applied for detailed evaluation of some kinetics factors obtained from the release data. Four different equations were used: zero-order equation, first-order equation, models: Korsmeyer–Peppas and Hixson–Crowell. Values of the determined half-time release for zero and first-order kinetic models ranged from 11.56 to 89.97 min. In the case of analysis according to these typical models, the values of the square root of the correlation coefficients were included between 0.9916 and 0.9995. The results transformed for the Hixson–Crowell model as constant release Ks, ranged between 0.0160 and 0.0437. The values of the respective calculated squares of the correlation coefficient ranged from 0.9933 to 0.9959. The determined release rate constants according to the Korsmeyer–Peppas model were between 0.0023 and 0.1630. The coefficients ‘n’ of the Korsmeyer–Peppas equation did not exceed 1.2 with the corresponding r2 values 0.9408–0.9960. Obtained results confirmed that the method is applicable for evaluation of selected drug compositions containing iron ions.


Author(s):  
Lorenzo Lisuzzo ◽  
Giuseppe Cavallaro ◽  
Stefana Milioto ◽  
Giuseppe Lazzara

AbstractIn this work, we investigated the effects of the vacuum pumping on both the loading efficiencies and the release kinetics of halloysite nanotubes filled with drug molecules dissolved in ethanol. As model drugs, salicylic acid and sodium diclofenac were selected. For comparison, the loading of the drug molecules was conducted on platy kaolinite to explore the key role of the hollow tubular morphology on the filling mechanism of halloysite. The effects of the pressure conditions used in the loading protocol were interpreted and discussed on the basis of the thermodynamic results provided by Knudsen thermogravimetry, which demonstrated the ethanol confinement inside the halloysite cavity. Several techniques (TEM, FTIR spectroscopy, DLS and $$\zeta$$ ζ -potential experiments) were employed to characterize the drug filled nanoclays. Besides, release kinetics of the drugs were studied and interpreted according to the loading mechanism. This work represents a further step for the development of nanotubular carriers with tunable release feature based on the loading protocol and drug localization into the carrier. Graphic abstract The filling efficiency of halloysite nanotubes is enhanced by the reduction of the pressure conditions used in the loading protocol.


2012 ◽  
Vol 8 (3) ◽  
Author(s):  
Xiaoyan Dai ◽  
Chenhuan Yu ◽  
Qiaofeng Wu

Abstract Jiangpo is an increasingly popular East Asian spice which is made from Mangnolia officinalis bark and ginger juice. Since it induces bioactive compounds decomposition and has influence on final flavor and fragrance, cooking is regarded as the key operation in preparation of Jiangpo. To evaluate the bioactive compounds content changes of Jiangpo during thermal processing, kinetic parameters including reaction order, rate constant, T1/2 and activation energy of bioactive markers namely honokiol, magnolol and curcumin were determined. Cooking was set at temperatures 60, 90 and 120 °C for selected time intervals. Results displayed the thermal kinetic characteristics of the three compounds. Thermal degradation of Honokiol and magnolol both followed first order kinetic model and the loss of curcumin fitted second order. A mathematical model based on the obtained kinetic parameters has also been developed to predict the degradation of honokiol, magnolol and curcumin in non-isothermal state. All the information in this paper could contribute necessary information for optimizing the existing heat processing of Jiangpo.


2008 ◽  
Vol 32 (2) ◽  
pp. 533-540 ◽  
Author(s):  
Vladimir Antônio Silva ◽  
Giuliano Marchi ◽  
Luiz Roberto Guimarães Guilherme ◽  
José Maria de Lima ◽  
Francisco Dias Nogueira ◽  
...  

Kinetic studies on soil potassium release can contribute to a better understanding of K availability to plants. This study was conducted to evaluate K release rates from the whole soil, clay, silt, and sand fractions of B-horizon samples of a basalt-derived Oxisol and a sienite-derived Ultisol, both representative soils from coffee regions of Minas Gerais State, Brazil. Potassium was extracted from each fraction after eight different shaking time periods (0-665 h) with either 0.001 mol L-1 citrate or oxalate at a 1:10 solid:solution ratio. First-order, Elovich, zero-order, and parabolic diffusion equations were used to parameterize the time dependence of K release. For the Oxisol, the first-order equation fitted best to the experimental data of K release, with similar rates for all fractions and independent of the presence of citrate or oxalate in the extractant solution. For all studied Ultisol fractions, in which K release rates increased when extractions were performed with citrate solution, the Elovich model described K release kinetics most adequately. The highest potassium release rate of the Ultisol silt fraction was probably due to the transference of "non-exchangeable" K to the extractant solution, whereas in the Oxisol exchangeable potassium represented the main K source in all studied fractions.


Holzforschung ◽  
2006 ◽  
Vol 60 (2) ◽  
pp. 137-142 ◽  
Author(s):  
Zhi-Hua Jiang ◽  
Jean Bouchard ◽  
Richard Berry

Abstract The finding that hexenuronic acid (HexA) groups can be selectively removed from kraft pulps by acid hydrolysis has provided an opportunity to reduce bleaching chemicals. However, there is evidence that the acid hydrolysis is not uniform. In this report, we evaluate the kinetics of acid hydrolysis of HexA in a xylan sample enriched with HexA, a conventional kraft pulp, and three modified kraft pulps: anthraquinone pulp (Kraft-AQ), polysulfide pulp (PS), and polysulfide-anthraquinone pulp (PS-AQ). We found that HexA present in the xylan and conventional kraft pulp behaved similarly toward the acid hydrolysis throughout. On the other hand, HexA present in the Kraft-AQ, PS-AQ and PS pulps was heterogeneous toward acid hydrolysis and the reaction can be separated into two pseudo-first-order kinetic phases, each of which has a different rate constant. The kinetic data provide evidence for the formation of lignin-HexA-xylan complexes during modified kraft pulping processes.


2012 ◽  
Vol 58 (No. 10) ◽  
pp. 471-476 ◽  
Author(s):  
H.R. Motaghian ◽  
A.R. Hosseinpur

The greenhouse experiment was performed to determine Cu release characteristics in the bulk and the rhizosphere of some calcareous soils using rhizobox. The kinetics of Cu release in the bulk and the rhizosphere soils were determined by successive extraction with diethylenetriaminepentaacetic acid-triethanolamine (DTPA-TEA) and 10 mmol/L citric acid in a period of 1 to 504 h at 25 ± 1°C. The results of kinetics study showed that Cu extracted using DTPA-TEA in the rhizosphere soils was significantly (P < 0.01) lower than the bulk soils, while Cu extracted using citric acid in the rhizosphere soils was significantly (P < 0.01) higher than the bulk soils. The mean of released Cu after 504 h using DTPA-TEA were 8.59 and 7.46 mg/kg in the bulk and the rhizosphere soils, respectively. The mean release of Cu after 504 h using citric acid was 14.73 and 16.05 mg/kg in the bulk and the rhizosphere soils, respectively. Release kinetics of Cu in two extractants conformed fairly well to parabolic diffusion, power function, and first order equations. The results of correlation analysis illustrated that a significant correlation between Cu desorption after 504 h with citric acid and Cu concentration in wheat was found (r = 0.96 and r = 0.90 in the rhizosphere and the bulk soils, respectively, P < 0.01). Therefore, application of 10 mmol/L citric acid extractant would be recommended in the future study on the kinetics of release of Cu in calcareous soils.  


2019 ◽  
Vol 115 (7/8) ◽  
Author(s):  
Samson N. Ugwu ◽  
Christopher C. Enweremadu

Emerging from the energy crisis of 2008 in South Africa, climate change concerns and the global desire to reduce high ozone-depleting emissions, renewable energy sources like biogas are gaining wide acceptance in most localities for heating and electricity. The paucity of feedstock varieties is a major challenge plaguing the sustainability of this sector. Biomethane potential, biodegradability and degradation kinetics of organic substrates are essential for assessing the suitability of feedstocks for methane generation and the overall performance of the anaerobic digestion process in biogas plants. Waste from the vegetable okra (Abelmoschus esculentus) is a novel substrate; its biodegradability and degradation dynamics in biomethane production are largely unstudied, and were therefore the aims of this research. The substrate was digested for 25 days at the mesophilic condition and the biomethane potential data were recorded. Measured data of methane yield and the elemental composition of the substrate were used to fit five models (modified Gompertz, Stannard, transference function, logistic and first-order models) to predict degradation parameters and determine biodegradability of the substrate, respectively. Low lag phase (0.143 d), positive kinetic constant (0.2994/d) and the model fitness indicator ( less than 10) showed that transference and first-order kinetic models predicted the methane yield better than did other growth functions. The experimental methane yield was 270.98 mL/gVS, theoretical methane yields were 444.48 mL/gVS and 342.06 mL/gVS and model simulation ranged from 267.5 mL/gVS to 270.89 mL/gVS. With a prediction difference of 0.03–1.28%, all growth functions acceptably predicted the kinetics of A. esculentus waste. The findings of this study offer information on this novel substrate important for its use in large-scale biogas production.


2014 ◽  
Vol 68 (1) ◽  
Author(s):  
Qamruzzaman ◽  
Abu Nasar

AbstractThe kinetics of the degradation of metribuzin by water-soluble colloidal MnO2 in acidic medium (HClO4) were studied spectrophotometrically in the absence and presence of surfactants. The experiments were performed under pseudo-first-order reaction conditions in respect of MnO2. The degradation was observed to be of the first order in respect of MnO2 while of fractional order for both metribuzin and HClO4. The rate constant for the degradation of metribuzin was observed to decrease as the concentration of MnO2 increased. The anionic surfactant, sodium dodecyl sulphate (SDS), was observed to be ineffective whereas the non-ionic surfactant, Triton X-100 (TX-100), accelerated the reaction rate. However, the cationic surfactant, cetyltrimethyl ammonium bromide (CTAB), caused flocculation with oppositely-charged colloidal MnO2; hence further study was not possible. The catalytic effect of TX-100 was discussed in the light of the available mathematical model. The kinetic data were exploited to generate the various activation parameters for the oxidative degradation of metribuzin by colloidal MnO2 in the absence as well as the presence of the non-ionic surfactant, TX-100.


Author(s):  
Xiping Nan ◽  
Shuli Nan ◽  
Xianpeng Zeng ◽  
Lining Kang ◽  
Xiangying Liu ◽  
...  

The inhibition kinetics of glutathione (GSH) and quercetin on Acrylamide (AA) formation in the low-moisture Maillard systems were investigated at 180 °C. The inhibition rates in an equal-molar asparagine/glucose (Asn/Glc) system was higher than those in asparagine/fructose (Asn/Fru) system, and the maximum inhibition rates for AA were 57.75% with GSH of 10 -2 mol L -1 and 51.38% with quercetin of 10 -1 mol L -1 . The Logistic-Index dynamic model and simplified two consecutive first-order kinetic models were well fitted to the changes of AA in the Asn/Glc system. The kinetics results suggested the predominant inhibition effect of GSH on AA could be attributed to the competitive reaction between GSH and Asn for the consumption of Glc. The kinetic results and HPLC-MS/MS analysis of quercetin inhibiting AA indicated that quercetin might mitigate AA through the binding reaction of quercetin decomposition product and Maillard intermediate product. These experimental results can provide theoretical data to control the formation of AA during food thermal processing.


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