scholarly journals Lipid Nanoparticles Loaded with Iridoid Glycosides: Development and Optimization Using Experimental Factorial Design

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3161
Author(s):  
Marta Dąbrowska ◽  
Eliana B. Souto ◽  
Izabela Nowak

Lipid nanoparticles based on multiple emulsion (W/O/W) systems are suitable for incorporating hydrophilic active substances, including iridoid glycosides. This study involved optimization of composition of lipid nanoparticles, incorporation of active compounds (aucubin and catalpol), evaluation of stability of the resulting nanocarriers, and characterization of their lipid matrix. Based on 32 factorial design, an optimized dispersion of lipid nanoparticles (solid lipid:surfactant—4.5:1.0 wt.%) was developed, predisposed for the incorporation of iridoid glycosides by emulsification-sonication method. The encapsulation efficiency of the active substances was determined at nearly 90% (aucubin) and 77% (catalpol). Regarding the stability study, room temperature was found to be the most suitable for maintaining the expected physicochemical parameter values (particle size < 100 nm; polydispersity index < 0.3; zeta potential > |± 30 mV|). Characterization of the lipid matrix confirmed the nanometer size range of the resulting carriers (below 100 nm), as well as the presence of the lipid in the stable β’ form.

2020 ◽  
Vol 10 (4) ◽  
pp. 404-418
Author(s):  
Kruti Borderwala ◽  
Ganesh Swain ◽  
Namrata Mange ◽  
Jaimini Gandhi ◽  
Manisha Lalan ◽  
...  

Background: The objective of this study was to develop solid lipid nanoparticles (SLNs) of poorly water soluble anti-hyperlipidemic drugs-Ezetimibe in combination with Simvastatin. Methods: This study describes a 32 full factorial experimental design to optimize the formulation of drug loaded lipid nanoparticles (SLN) by the high speed homogenization technique. The independent variables amount of lipid (GMS) and amount of surfactant (Poloxamer 188) were studied at three levels and arranged in a 32 factorial design to study the influence on the response variables- particle size, % entrapment efficiency (%EE) and cumulative drug release (% CDR) at 24 h. Results: The particle size, % EE and % CDR at 24 h for the 9 batches (B1 to B9) showed a wide variation of 104.6-496.6 nm, 47.80-82.05% (Simvastatin); 48.60-84.23% (Ezetimibe) and 54.64-92.27% (Simvastatin); 43.8-97.1% (Ezetimibe), respectively. The responses of the design were analysed using Design Expert 10.0.2. (Stat-Ease, Inc, USA), and the analytical tools of software were used to draw response surface plots. From the statistical analysis of data, polynomial equations were generated. Optimized formulation showed particle size of 169.5 nm, % EE of 75.43% (Simvastatin); 79.10% (Ezetimibe) and 74.13% (Simvastatin); 77.11% (Ezetimibe) %CDR after 24 h. Thermal analysis of prepared solid lipid nanoparticles gave indication of solubilisation of drugs within lipid matrix. Conclusion: Fourier Transformation Infrared Spectroscopy (FTIR) showed the absence of new bands for loaded solid lipid nanoparticles indicating no interaction between drugs and lipid matrix and being only dissolved in it. Electron microscope of transmission techniques indicated sphere form of prepared solid lipid nanoparticles with smooth surface with size approximately around 100 nm.


2016 ◽  
Vol 8 ◽  
pp. 60
Author(s):  
Pawar Anil R. ◽  

ENHANCEMENT OF AQUEOUS SOLUBILITY OF EZOGABINE: PREPARATION AND CHARACTERIZATION OF EZOGABINE NANOSUSPENSION ANTICIPATED FOR NOSE TO BRAIN TARGETING BY 32 FACTORIAL DESIGN


INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (05) ◽  
pp. 14-24
Author(s):  
G. S Bangale ◽  
◽  
K. S. Rajesh ◽  
G.V. Shinde

The objective of the present study was to develop nano range liposomal formulation for cancer therapy and optimize the formulation by response surface method, i.e. 32 factorial design, in order to minimize more efforts, time and material use when formulation like the liposomes are developed. Two independent variables, namely, the concentration of lipid (X1) and the concentration of cholesterol (X2), were set at three different levels. High and low levels of each variable were coded as 1 and -1, respectively, and the mean value was coded as zero. The dependent variables for factorial batches measured as vesicle size (Y1) was 61.5 to 72.3%, and % encapsulation efficiency (Y2) was found to be 127 to 240 nm. Stepwise regression analysis was used to find out the control factors that significantly affect response variables. The results were subjected to ANOVA and multiple regression analysis that led to equations describing the effect of independent variables on the selected responses. The level of significance selected was 5% (p<0.05). Contour plot and response surface plot were constructed & overlay plot was used to optimize the formulation by keeping the desired responses. The optimized formulation CL-10 has vesicle size of 132 nm & PDI value of 0.241. Zeta potential of formulation was -20.4, conforming the formulations stability. Vesicular morphology measured by SEM & TEM study indicates that the vesicle was spherical in nature. Stability study of optimized formulation was carried out for 6 months as per ICH guidelines at 40C and 370C and indicates no significant changes in parameters like % drug release, vesicle size, % EE supported by student t test (p=0.05).


Author(s):  
Vipul K. Sapavadiya ◽  
Miral V. Sapavadiya ◽  
Pragna K. Shelat ◽  
Anita N. Lalwani

Granisetron is a highly selective serotonin (5-HT3) receptor blocker which prevents the vomiting reflex induced by serotonin during cancer chemotherapy. The objective of present research work was development and optimization of mouth dissolving film of granisetron hydrochloride. Solvent casting method was used for preparation of mouth dissolving film. Various film forming polymers like PVP K-30, PVA, maltodextrin, HPMC E5 LV and lycoat RS 720 along with and plasticizer like Propylene glycol, Poly ethylene glycol 400 and glycerin were used for selection of suitable polymer plasticizer combination. Film prepared using lycoat RS 720 and PEG-400 was found satisfactory and further factorial design and desirability function was used for optimization. Regression equation and counter plots were executed to dependent variables i.e., tensile strength, % elongation, elastic modulus and % drug release in 1 minutes to independent variables. Results of experimental design revealed that the independent factors lycoat RS 720 and PEG-400 significantly influenced the mechanical properties and % drug release from the film which was ultimately reflected in this formulation of optimized batch. All experimental design formulations were evaluated for weight variation, thickness, drug content, % moisture loss, pH, folding endurance and stability study at 40˚ ± 2˚ C/75 ± 5% RH. From the result of optimized batch it can be concluded that an optimized formulation was stable with suitable packaging and the high % drug release of film in simulated saliva indicate that it can be used for drug delivery system of granisetron hydrochloride having first pass metabolism


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