scholarly journals Preparation, Characterization, and Pharmacokinetic Evaluation of Imperatorin Lipid Microspheres and Their Effect on the Proliferation of MDA-MB-231 Cells

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 236 ◽  
Author(s):  
Xinli Liang ◽  
Xulong Chen ◽  
Guowei Zhao ◽  
Tao Tang ◽  
Wei Dong ◽  
...  
Keyword(s):  
Particle Size ◽  
Response Surface ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Experimental Conditions ◽  
Zeta Potentials ◽  
Preparation Conditions ◽  
Egg Lecithin ◽  
Central Composite ◽  
Lipid Microsphere

Imperatorin is a chemical compound belonging to the linear furanocoumarins. Imperatorin is attracting considerable attention because of its antitumor, antibacterial, anti-inflammatory, and anticoagulant activities, inhibition of myocardial hypertrophy, and other pharmacological efficacies. However, imperatorin has limited water solubility and has better lipid solubility; thus, we decided to design and synthesize imperatorin lipid microspheres to optimize the preparation conditions. The aim was to develop and formulate imperatorin lipid microspheres through nanoemulsion technology and apply the response surface–central composite design to optimize the imperatorin lipid microsphere formulation. The influence of the amounts of egg lecithin, poloxamer 188, and soybean oil for injection on the total percentage of the oil phase was investigated. The integrated effect of dependent variables, including particle size, polydispersity index, zeta potentials, drug loading, and encapsulation efficiency, was investigated. Data of overall desirabilities were fitted to a second-order polynomial equation, through which three-dimensional response surface graphs were described. Optimum experimental conditions were calculated by Design-Expert 8.06. Results indicated that the optimum preparation conditions were as follows: 1.39 g of egg lecithin, 0.21 g of poloxamer 188, and 10.57% soybean oil for injection. Preparation of imperatorin lipid microspheres according to the optimum experimental conditions resulted in an overall desirability of 0.7286, with the particle size of 168 ± 0.54 nm, polydispersity index (PDI) of 0.138 ± 0.02, zeta potentials of −43.5 ± 0.5 mV, drug loading of 0.833 ± 0.27 mg·mL−1, and encapsulation efficiency of 90 ± 1.27%. The difference between the observed and predicted values of the overall desirability of the optimum formulation was in the range from 2.4% to 4.3%. Subsequently, scanning electron microscopy was used to observe the micromorphology of the imperatorin lipid microspheres, showing round globules of relatively uniform shape and sizes within 200 nm. The effect of imperatorin lipid microspheres on MDA-MB-231 proliferation was investigated by the MTT method. Furthermore, pharmacokinetics in Sprague-Dawley rats was evaluated using orbital bleeding. A sensitive and reliable liquid chromatography with the high-performance liquid chromatography (HPLC) method was established and validated for the quantification of imperatorin in rat plasma samples. The data were calculated by DAS (drug and statistics) Pharmacokinetic Software version 3.3.0 (Version 3.3.0, Shanghai, China). Results demonstrated that imperatorin lipid microspheres can significantly enhance the bioavailability of imperatorin and can significantly inhibit MDA-MB-231 cell proliferation. In conclusion, our results suggested that the response surface–central composite design is suitable for achieving an optimized lipid microsphere formulation. Imperatorin lipid microspheres can improve the bioavailability of imperatorin and better inhibit the proliferation of MDA-MB-231 cells as compared to imperatorin alone.

scholarly journals Preparation, Characterization and Pharmacokinetics Evaluation of Imperatorin Lipid Microsphere and Its Effect on Proliferation of MDA-MB-231

2018 ◽  
Author(s):  
Xinli Liang ◽  
Xulong Chen ◽  
Guowei Zhen ◽  
Tao Tang ◽  
Chunyan Wang ◽  
...  
Keyword(s):  
Liquid Chromatography ◽  
Response Surface ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Experimental Conditions ◽  
Zeta Potentials ◽  
Preparation Conditions ◽  
Egg Lecithin ◽  
Central Composite ◽  
Lipid Microsphere

Imperatorin is a chemical compound belong to Linear furan coumarins. Imperatorin is attracting considerable attention because of its anti-tumor, antibacterial, anti-inflammatory, anticoagulant and inhibition of myocardial hypetrophy and other pharmacological efficacy. However, imperatorin has limited water solubility and preferable lipid solubility, we decided to design and synthesize imperatorin lipid microsphere, to optimize preparation conditions. The aim was to develop and formulate imperatorin lipid microsphere through nano emulsion technology and apply the response surface-central composite design to optimize the imperatorin lipid microsphere formulation. Influence of content of amount of egg lecithin(A), amount of poloxamer188(B), soybean oil for injection accounted for the total percentage of oil phase(C) were investigated. Integrated effect of dependent variables including particle size(Y1), polydispersity index(Y2), Zeta potentials(Y3), drug loading(Y4), encapsulation efficiency(Y5). Data of overall desirabiities were fitted to a second-order polynomial equation, through which three dimensional response surface graphs were described. Optimum experimental conditions were calculated by Design-Expert 8.06. Results indicated that the optimum preparation conditions were as follows: egg lecithin amount 1.39 g, poloxamer188 amount 0.21 g, soybean oil for injection amount 10.57%. Preparation of imperatorin lipid microsphere according to the optimum experimental conditions resulted in an overall desirability of 0.7286, while the particele size (168±0.54) nm, polydispersity index (PDI) (0.138±0.02), Zeta potentials (−43.5±0.5) mV, drug loading (0.833±0.27) mg·mL−1, encapsulation efficiency (90±1.27)%. The difference between observed and predicted values of the overall desirability of the optimum formulation was in range from 2.4% to 4.3%. Subsequently, using the Scanning electron microscopy to observe the micromorphology of imperatorin lipid microsphere, the result shows that round globular of relatively uniform and sizes within 200nm.The proliferation study of imperatorin lipid microsphere on MDA-MB-231 was investigated by MTT method. Furthermore, pharmacokinetics in Sprague Dawley rats were evaluated using orbital bleeding. A sensitive and reliable liquid chromatography with High Performance Liquid Chromatography (HPLC) method was established and validated for the quantification of imperatorin in rat plasma samples. The data were calculated by DAS (Drug and statistics) pharmacokinetic software version3.2.6 (China). Results demonstrated that imperatorin lipid microsphere can significantly enhance the bioavailability of imperatorin and can significantly inhibit MDA-MB-231 cell proliferating. In conclusion, our results suggersted that the response surface-central composite design is suitable for the optimized lipid microspere formulation. Imperatorin Lipid microsphere can improve the bioavailability of imperatorin and inhibit the proliferation of MDA-MB-231 than that of imperatorin.

Application Research of Lipid Microsphere Biological Carrier Material on Prescription of Tanshinone II a Lipid Microsphere by Central Composite Design-Response Surface Method

2015 ◽  
Vol 1120-1121 ◽  
pp. 834-841
Author(s):  
Xin Li Liang ◽  
Dan Lv ◽  
Juan Luo ◽  
Xue Jing Guan ◽  
Zheng Gen Liao
Keyword(s):  
Response Surface ◽  
Encapsulation Efficiency ◽  
Average Particle Size ◽  
Egg Yolk ◽  
Tanshinone Iia ◽  
Average Particle ◽  
Surface Method ◽  
Size Stability ◽  
Central Composite ◽  
Lipid Microsphere

To optimize the prescription of tanshinone IIA lipid microspheres by central composite design method, and evaluate the quality. Through evaluating average particle size, stability constant and the encapsulation efficiency of the lipid microsphere to investigate the concentration of the egg yolk lecithin and the poloxamer and the percentage of Soybean oil in the total oil phase which may impact the properties of tanshinone IIA lipid microsphere. Building the mathematic relation between the index and factor by the binomial expression, according to the best mathematical model of the evaluation indicators to describe response surface and then to use response surface method to predict the best prescription which will be analysed. According to the prescription optimization to prepare tanshinone IIA lipid microsphere and evaluate its quality. The results showed that each index of the binomial equation fitting is good, the correlation coefficient of the average particle size, stability constant and the encapsulation efficiency are 0.97, 0.92 and 0.84 respectively. The optimized prescription is as follows: egg yolk lecithin1.38 g, F68 0.19 g, LCT 2 g, MCT 18 g, all the indexes of the optimized prescription are similar to the target values.

Simultaneous Incorporation of 5-Fluorouracil and Leucovorin into Chitosan Nanoparticle as Drug Carrier and Its Characterization

2010 ◽  
Vol 654-656 ◽  
pp. 2265-2268
Author(s):  
Pu Wang Li ◽  
Yi Chao Wang ◽  
Zheng Peng ◽  
Ling Xue Kong
Keyword(s):  
Particle Size ◽  
Strong Interaction ◽  
Encapsulation Efficiency ◽  
Drug Carrier ◽  
Drug Loading ◽  
Anti Cancer ◽  
Chitosan Nanoparticle ◽  
Combined Drugs ◽  
Drug Encapsulation Efficiency ◽  
Interaction Between Drugs

A combined drug loaded system containing two most common anti-cancer drugs 5-fluorouracil (5-FU) and leucovorin (LV) was designed and prepared by ion crosslinking technology. The resulted nanoparticles are spherical in shape, and the particle size becomes larger when drug combination are loaded. Efficient drug encapsulation efficiency (EE) and drug loading (LC) are obtained due to the strong interaction between drugs and polymer. The combined drugs are distributed in the particles in amorpholous state which are demonstrated by the XRD results.

scholarly journals Sodium Alginate Nanoparticles of Isoniazid: Preparation and Evaluation

2019 ◽  
Vol 11 (06) ◽  
Author(s):  
Sumit Kumar ◽  
Dinesh Chandra Bhatt
Keyword(s):  
Particle Size ◽  
Sodium Alginate ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Average Particle Size ◽  
Average Particle ◽  
In Vitro Drug Release ◽  
Ionotropic Gelation ◽  
Preparation And Evaluation

Fabrication and evaluation of the Isoniazid loaded sodium alginate nanoparticles (NPs) was main objective of current investigation. These NPs were engineered using ionotropic gelation technique. The NPs fabricated, were evaluated for average particle size, encapsulation efficiency, drug loading, and FTIR spectroscopy along with in vitro drug release. The particle size, drug loading and encapsulation efficiency of fabricated nanoparticles were ranging from 230.7 to 532.1 nm, 5.88% to 11.37% and 30.29% to 59.70% respectively. Amongst all batches studied formulation F-8 showed the best sustained release of drug at the end of 24 hours.

scholarly journals Formulation of Solid Lipid Nanoparticles of Cilnidipine for the Treatment of Hypertension

2019 ◽  
Vol 9 (3) ◽  
pp. 212-221 ◽  
Author(s):  
Aparna Bhalerao ◽  
Pankaj Prakash Chaudhari
Keyword(s):  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Lipid Nanoparticles ◽  
Water Soluble ◽  
Solid Lipid Nanoparticle ◽  
Solid Lipid ◽  
Lipid Nanoparticle

Cilinidipine is a fourth generation N and L-type calcium channel antagonists used alone or in combination with another drug to treat hypertension. Cilnidipine is poorly water -soluble, BCS class II drug with 6 to 30 percent oral bioavailability due to first pass metabolism. So to protect the drug from degradation and improve its dissolution, solid lipid nanoparticles were prepared. Glyceryl monostearate was selected as lipid while span 20: tween 20 were selected as surfactant blends. The formulations were evaluated for various parameters, as percent transmittance, drug content, percent encapsulation efficiency; percent drug loading, In vitro drug release and particle size. Optimized formulation was lyophilized using lactose as a cryo-protectant. The lyophilized formulation was evaluated for micromeritic properties, particle size and in vitro dissolution. It was further evaluated for DSC, XRD, and SEM. Percent encapsulation efficiency and percent drug loading of optimized formulation (F3) were 78.66percent and 9.44percent respectively. The particle size of F3 formulation without drug was 204 nm and with the drug was 214 nm. The particle size of the reconstituted SLN was 219 nm. In DSC study, no obvious peaks for cilnidipine were found in the SLN of cilnidipine indicated that the cilnidipine must be present in a molecularly dissolved state in SLN. In X-ray diffractometry absence of peaks representing crystals of cilnidipine in SLN indicated that the drug was in an amorphous or disordered crystalline phase in the lipid matrix. Thus, solid lipid nanoparticle formulation is a promising way to enhance the dissolution rate of cilnidipine. Keywords: Cilnidipine, Solid Lipid Nanoparticle, Hypertension

scholarly journals Preparation and pharmacokinetics of genistein MePEG-PLGA copolymer micelles

2019 ◽  
Author(s):  
Mina Swartz ◽  
John Smith
Keyword(s):  
Particle Size ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Weibull Model ◽  
Pharmacokinetic Parameters ◽  
Release Behavior ◽  
Concentration Data ◽  
Tail Vein ◽  
Initial Stability ◽  
Copolymer Micelles

AbstractIn this report, we demonstrated a novel technique to prepare genistein (GEN) MePEG-PLGA copolymer micelles. Initial stability and pharmacokinetic behavior in rats after intravenous administration were investigated. The micelles were prepared by modified self-emulsifying solvent evaporation method. The morphology, encapsulation efficiency, drug loading, particle size and Zeta potential were investigated. The release behavior was investigated by dynamic membrane dialysis technique. The micelles were stored in a refrigerator at 4 °C, and samples were taken after 1 d, 10 d, 1 month, 3 months, and 6 months, and the encapsulation efficiency and drug loading were examined. The GEN micelles were injected into the tail vein of healthy rats. The blood concentration of GEN in rats was determined by HPLC. The plasma concentration data was processed by DAS 2.0 software. The main pharmacokinetic parameters were statistically analyzed by SPSS 17.0 software. Results The encapsulation efficiency of the prepared micelles was (84.43+/-2.93) %, the drug loading was (2.63+/-0.91) %, and the particle size was (63.75+/-4.12) nm. The release behavior of GEN micelles was in line with the Weibull model. The 6-month leakage rate of GEN micelles was 2.45%, and the drug loading decreased by 0.18%. The main pharmacokinetic parameters AUC0-t after GEN micelles and GEN emulsion 40 mg·kg-1 were injected into the tail vein of rats. They were (99.46+/- 4.77) mg · L-1 ·h and (57.51+/-1.37) mg·L-1 ·h, and t1/2 were (7.48+/-1.15)h and (4.95+/- 1.15)h, respectively, and Cmax was (16.03+/-1.20) mg·L-1 and (16.73+/-1.10) mg·L-1, CL are (0.36+/-0.02) L·h-1 ·kg-1 and (0.67+/-0.02)L·h-1 ·kg-1.

scholarly journals Nanoencapsulation and identification of phenolic compounds by UPLC-Q/TOF-MS2 of an antioxidant extract from Opuntia atropes

2020 ◽  
Vol 10 (12) ◽  
pp. 505
Author(s):  
Héctor E. Martínez-Flores ◽  
Eunice Tranquilino-Rodríguez ◽  
José O. Rodiles-López ◽  
Guillermo C. G. Martínez-Avila
Keyword(s):  
Particle Size ◽  
Phenolic Acids ◽  
Encapsulation Efficiency ◽  
Soy Protein Isolate ◽  
Polyphenolic Compounds ◽  
Wall Material ◽  
Process Conditions ◽  
Experimental Conditions ◽  
Feeding Speed ◽  
Polyphenolic Profile

Background: Nanoencapsulation is a technique that protects bioactive compounds such as polyphenolic compounds from environmental factors, through a biopolymer that acts as a wall system. Cladodes of O. atropes are an important source of polyphenolic compounds, flavonoids being the most abundant, these are mainly in the form of glycosides and their consumption has been related to a decrease in glucose and lipid profile through the elimination of intracellular radicals.Purpose of the study: To study the formulation and process parameters that allow obtaining the best experimental conditions to nanoencapsulation and protect the polyphenolic compounds of the O. atropes extract.Methods: Wall materials applied for nanoencapsulation (soy protein isolate, calcium caseinate , and maltodextrin). A Box Behnken 33 design was used; wall material extract of O. atropes (1/1, 2.5 / 1, 4/1), temperature (95, 105 and 115 ° C) and spray (40, 70 and 100%), to evaluate the yield, feeding speed, particle size, encapsulation efficiency, phenolic acids, flavonoids, DPPH• and ABTS•+. Polyphenolic compounds were identified by UPLC-Q / TOF-MS2.Results: Maltodextrin presented better properties in the encapsulation of the extract of O. atropes. The Box Behnken 33 design made it possible to identify the treatment with the appropriate quality characteristics for the nanoencapsulation process; Formulation 2.5 / 1 (maltodextrin / O. atropes extract), 115 ° C and 100% spray, to obtain 85.22% yield, feeding speed of 9 mL / h, the particle size of 154.77 nm, 55.69 % encapsulation efficiency, phenolic acids of 0.95 mg GAE / g, flavonoids of 7.02 mg QE / g, and antioxidant activity in DPPH• of 0.29 mg GAE / g and  ABTS•+ of 0.45 mg GAE / g. The polyphenolic profile was characterized, and it was confirmed that nanoencapsulation protects some isomers of isorhamnetin 3-O-rhamnosido-7-O- (rhamnosyl-hexoside) and p-coumaric acid 4-O-glucoside.Conclusion: Maltodextrin is an excellent encapsulating material of the O. atropes extract, the formulation and process conditions that favored all the response variables were identified and it was shown that nanoencapsulation protects the polyphenolic compounds.Keywords: O. atropes extract, nanoencapsulation, polyphenolic profile, UPLC-Q / TOF-MS2.

Liposomal Mediated Carriers of α Lipoic Acid for the Treatment of Acute Lung Injury: Preclinical Study in Rat Model

2020 ◽  
Vol 10 (1) ◽  
pp. 53-57
Author(s):  
Yu Cao ◽  
Yanling Chai ◽  
Xiaoqun Niu ◽  
Bing Hai ◽  
Xiaojie He ◽  
...  
Keyword(s):  
Thin Film ◽  
Particle Size ◽  
Pulmonary Fibrosis ◽  
Lung Injury ◽  
Lipoic Acid ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Preclinical Study ◽  
Liposomal Formulation ◽  
Experimental Animals

The present investigation deals with formulation of lipoic acid as liposomal formulation and to evaluate its efficacy in Lung injury (Pulmonary Fibrosis). The liposomal formulation of Lipoic acid (LA-liposomes) was successfully prepared by thin film hydration method. Such prepared liposomes were characterized for particle size, encapsulation efficiency, drug loading etc. characteristic. An Pulmonary fibrosis was induced using Bleomycin experimental animals rats. The effect of LA liposomal formulation on pulmonary fibrosis was observed. The histopathological finding confirms the efficiency of formulation in attenuation of pulmonary fibrosis.

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