Application of statistical experimental design to study the formulation variables influencing the coating process of lidocaine liposomes

González-Rodrı́guez, Marı́a Luisa; Barros, Lorena; Palma, Juan Luis; González-Rodríguez, P.L.; Rabasco, A. M.

doi:10.1016/j.ijpharm.2007.01.024

Cited by 91 publications

(42 citation statements)

References 30 publications

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“…Contrasting results are reported in literature about the effect of CS coating on the vesicle entrapment efficiency, depending on the nature of the entrapped drug. In a previous work, some of us observed a negative effect of CS concentration on lidocaine encapsulation capacity of liposomes (González-Rodríguez et al, 2007). This result was attributed to a competition between the lidocaine and CS molecules (both ionized at the pH 5.0 of experimental conditions), for interaction with phosphatidylcholine, which hindered drug retention into the vesicles (González-Rodríguez et al, 2007).…”

Section: Chitosomespreparation and Characterizationmentioning

confidence: 93%

“…Samples were submitted to five vortex cycles (each consisting in 2 min stirring and 5 min heating at 58 C) until vesicle formation. The temperature was maintained at 58 C (above the gel-liquid transition temperature of the amphiphilic and lipid substances) until the end of the process.For vesicle coating with CS, the liposomal sample was added drop wise (0.67 mL/min) at room temperature, under constant stirring rate (100 rpm), into 10 mL of a CS solution (0.1-0.4-0.7% w/v in 0.5% v/v glacial acetic acid solution) followed by incubation, under stirring, for 1 h at 10 C (González-Rodríguez et al, 2007). The final MTF concentration in the chitosomes was 3 mg/mL.…”

Section: Preparation Of Colloidal Dispersionsmentioning

confidence: 99%

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Calcium alginate microspheres containing metformin hydrochloride niosomes and chitosomes aimed for oral therapy of type 2 diabetes mellitus

Maestrelli

Mura

González-Rodrı́guez

et al. 2017

International Journal of Pharmaceutics

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Section: Chitosomespreparation and Characterizationmentioning

confidence: 93%

Section: Preparation Of Colloidal Dispersionsmentioning

confidence: 99%

Calcium alginate microspheres containing metformin hydrochloride niosomes and chitosomes aimed for oral therapy of type 2 diabetes mellitus

Maestrelli

Mura

González-Rodrı́guez

et al. 2017

International Journal of Pharmaceutics

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“…González-Rodrίguez et al applied experimental statistics to study the formulation variables influencing the coating process of lidocaine hydrochloride (LID) liposomes by chitosan [125]. These variables were the concentration of the chitosan coating solution, the dripping rate of this solution on the liposome colloidal dispersion, the stirring rate, the time elapsing since the production of liposomes for the liposome coating and finally the amount of drug entrapped in the liposomes.…”

Section: Influence Of the Preparation Techniques Of Chitin/chitosan-bmentioning

confidence: 99%

Biomedical Activity of Chitin/Chitosan Based Materials—Influence of Physicochemical Properties Apart from Molecular Weight and Degree of N-Acetylation

et al. 2011

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Abstract:The physicochemical nature of chitin and chitosan, which influences the biomedical activity of these compounds, is strongly related to the source of chitin and the conditions of the chitin/chitosan production process. Apart from widely described key factors such as weight-averaged molecular weight (M W ) and degree of N-acetylation (DA), other physicochemical parameters like polydispersity (M W /M N ), crystallinity or the pattern of acetylation (P A ) have to be taken into consideration. From the biological point of view, these parameters affect a very important factor-the solubility of chitin and chitosan in water and organic solvents. The physicochemical properties of chitosan solutions can be controlled by manipulating solution conditions (temperature, pH, ionic strength, concentration, solvent). The degree of substitution of the hydroxyl and the amino groups or the degree of quaternization of the amino groups also influence the mechanical and biological properties of chitosan samples. Finally, a considerable research effort has been directed towards developing safe and efficient chitin/chitosan-based products because many factors, like the size of nanoparticles, can determine the biomedical characteristics of medicinal products. The influence of these factors on the biomedical activity of chitin/chitosan-based products is presented in this report in more detail. OPEN ACCESSPolymers 2011, 3 1876

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“…For the preparation of chitosan-coated liposomes, 0.1% and 0.6% (w/v) chitosan solutions were prepared in 0.1% (v/v) glacial acetic acid 25 . A volume of 2.0 mL of chitosan solution was added drop-wise to the 2.0 mL of liposomes under magnetic stirring at room temperature for 1 hour, followed by incubation in refrigerator overnight.…”

Section: Chitosan Coatingmentioning

confidence: 99%

Mucoadhesive liposomal delivery systems: the choice of coating material

Karn

Vanić

Pepić

et al. 2010

Drug Development and Industrial Pharmacy

121

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Objective: Development of liposomal mucoadhesive drug delivery system, which is able to improve the bioavailability of poorly absorbed oral drugs by prolonging their gastric and intestinal residence time, through facilitating the intimate contact of the delivery system with the absorption membrane. Materials and methods: Liposomes containing model drug atenolol were prepared by the modified ethanol injection method. Liposomes containing atenolol were coated by different mucoadhesive polymers, for example, chitosan, Carbopol 974P, Eudragit L100, and Eudragit S100, to optimize the choice of coating material. The delivery systems were tested for their in vitro mucoadhesiveness. Results: Liposomes prepared by the ethanol injection method were of satisfactory size (around 100 nm, before coating). Through the coating of liposomes in the presence of unentrapped material, the entrapment efficiency for drug was increased. In vitro mucoadhesive test confirmed the mucoadhesive properties of the coated layer for all tested polymers; however, Eudragit S100-coated liposomes were superior to other coating materials. Discussion: Eudragit coating appeared to be an optimal polymer choice. These preliminary data indicate that polymer-coated mucoadhesive liposomes are able to carry sufficient amount of drug and to remain attached to the intestinal mucosa for a sufficient period of time to enable prolonged absorption of entrapped drug. Conclusion: While keeping in mind that the in vivo conditions may vary with the in vitro ones, we may recommend the system described in our work for possible oral delivery of peptides and phytochemicals.

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Application of statistical experimental design to study the formulation variables influencing the coating process of lidocaine liposomes

Cited by 91 publications

References 30 publications

Calcium alginate microspheres containing metformin hydrochloride niosomes and chitosomes aimed for oral therapy of type 2 diabetes mellitus

Calcium alginate microspheres containing metformin hydrochloride niosomes and chitosomes aimed for oral therapy of type 2 diabetes mellitus

Biomedical Activity of Chitin/Chitosan Based Materials—Influence of Physicochemical Properties Apart from Molecular Weight and Degree of N-Acetylation

Mucoadhesive liposomal delivery systems: the choice of coating material

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