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Abstract Hesperidin is a natural compound which is found in citric fruits and presents antitumor and antimicrobial activities. However, the in vivo efficacy of Hesperidin is reduced due to its low oral bioavailability. Protein-based nanoparticles have been applied to improve biological parameters of drugs and natural compounds. Gliadin is a monomeric protein present in wheat. In this study, gliadin-based nanoparticles containing hesperidin were obtained by desolvation technique and a Taguchi orthogonal array design was employed to optimize the formulation. The independent variables were set as concentration of CaCl2 (0.5; 1 or 2%) and stabilizing agent (Pluronic F68, Tween 80 or sodium caseinate). The dependent variables consisted of mean diameter, polydispersity index, zeta potential, and encapsulation efficiency. The results showed significant effects on the dependent variables when 1% CaCl2 and Pluronic F68 were used. The optimized formulation was coated with chitosan to increase the physical stability of the nanoparticles. The final nanoparticles presented a mean diameter of 321 nm and polydispersity index of 0.217, and spherical shape. After coating, the Zeta potential was +21 mV, and the encapsulation efficiency was 73 %. The in vitro release assay showed that about 98% of the drug was released from the nanoparticles after 48 h. Moreover, the nanoparticles reduced hesperidin cytotoxicity on healthy cells (Vero cells) and improved the cytotoxicity on tumor cells (HeLa, PC-3 and Caco-2 cells). Results showed that the chitosan-coated gliadin nanoparticles are potential carriers for hesperidin delivery for cancer treatment.
Assuntos
Quitosana/química , Gliadina/química , Hesperidina/farmacologia , Neoplasias/tratamento farmacológico , NanopartículasRESUMO
The present article utilized analytical quality by design (AQbD) methodology to optimize chromatographic conditionsfor the routine analysis of Cholecalciferol (CHL). Taguchi orthogonal array design and Box–Behnken designwere employed to screen and optimize critical method parameters for augmenting the method performance. Theoptimal chromatographic separation was attained on Eurosphere® 100-5, C8 (250 × 4.6 mm i.d., 5 μm) column in anisocratic elution mode using methanol:acetonitrile (50:50, % v/v) as mobile phase at a flow rate of 1.0 ml/minutesand photodiode array detection at 265 nm. The optimized chromatographic method was successfully validated asper International Council for Harmonisation Q2 (R1) guidelines. The method was found to be linear (r2 = 0.9993)in the range of 20–100 IU/ml. Limit of detection and limit of quantitation were found to be 10 and 20 IU/ml. Theprecision, robustness, and ruggedness values were within the acceptance limits (relative standard deviation < 2). Thepercent recovery of in-house developed 400 IU mouth dissolving tablets and marketed Tayo 60k tablets were foundto be 99.89% and 101.46%, respectively. The forced degradation products were well resolved from the main peaksuggesting the stability-indicating the power of the method. In conclusion, the AQbD-driven method is highly suitablefor analysis of CHL in bulk and pharmaceutical formulations
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Lamotrigine a BCS class II drug used in treatment of epilepsy has several disadvantages when taken orally (first pass metabolism and increased Cmax). The aim of the study is to design core in cup (In lay) buccoadhesive tablets which aims for controlled, unidirectional release, increased patient compliance and decreased side effects. The present study involves the preparation of core in cup tablets containing release retarding polymers like sodium alginate, xanthan gum and HPMC E 15LV in core and HPMC K 15M in cup for mucoadhesion. L9 orthogonal array Taguchi design was constructed for the study. The dependent variable studied for L9 orthogonal array Taguchi runs include % drug release from which the formulation with highest S/N ratio was optimized. All the runs were evaluated for physical parameters, drug release, mucoadhesive studies and assay. L1, L2, L4 and L8 formulations showed controlled release for up-to 8 hours with good assay values. The model dependent kinetics showed zero order kinetics with super case II transport and Hixson Crowell mechanism which indicates unidirectional drug release.
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Objective To establish a rapid and effective supercritical fluid extraction (SFE) and rapid resolution liquid chromatography method coupled with diode-array detector (RRLC-DAD) to quantify the chromones in a species. Methods The effects of four parameters including ethanol concentration (50%–90%), pressure (25–45 MPa), temperature (40–60 oC), and time (30–90 min) on the chromones yields, namely prim-O-glucosylcimifugin, cimifugin, 5-O-methylvisammioside, and sec-O-gluco-sylhamaudol, were investigated using SFE system with orthogonal array design (OAD). Furthermore, the extracts were analyzed using rapid resolution liquid chromatography coupled with diode-array detector (RRLC-DAD) system to confirm the results. Results Under the optimized conditions, i. e., 35 MPa of pressure, 60 °C of temperature, 70% ethanol, and 60 min of time, the yields of prim-O-glucosylcimifugin, cimifugin, 5-O-methylvisammioside, sec-O-glucosylhamaudol, and total chromones were 3.514, 0.132, 6.242, 0.342, and 10.231 mg/g, respectively. In comparison with ultrasonic assisted extraction (UAE), SFE was able to yield a 20.7% increase in the total chromones from Saposhnikoviae Radix. Conclusion SFE is an alternative and promising method to extract chromones from this species, and the established RRLC-DAD method could serve as a rapid and effective method for the identification of chromones from Saposhnikoviae Radix.
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Objective To investigate the optimal extraction technique and antioxidant activity of curcuminoids from Curcuma longa L. Methods The optimized extraction process of curcuminoids from Curcuma longa L. with ethanol as extracting solvent were studied based on orthogonal test.The effect of each factor such as the ethanol concentration, the amount of solvent, extraction temperature and extraction time were investigated based on a single-factor experiment.The effects of extraction yield of curcuminoids under different processing conditions were compared by HPLC method. Content of curcuminoids and antioxidant activity of the extract were used as comprehensive survey index. Free radical scavenging DPPH method was used to assess the antioxidant effect. And the extraction technique parameters were optimized. Results The condition of optimal extraction technique was: ethanol concentration 60%, amount of solvent 20 folds, extraction time 2 h, extraction temperature 90 ℃. Under these conditions, the extraction yield of curcuminoids was 3. 65%. DPPH free radical scavenging yield of the curcumin extract was 79.79%. Conclusion This optimized technology is simple and have a good reappearing rate, and the extracts of Curcuma longa L.show good antioxidant activity.
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Spectrophotometry and single factor test were used in the investigation of effects on extraction results of total flavonoids from the fruit ofVernonia esculenta Hemsl. from aspects of ethanol concentration, frequency of extraction, length of extraction time, and the solid-liquid ratio. The extraction conditions were optimized by orthogonal test. The results showed that the optimum extraction conditions were ethanol concentration of 70%, extracted for 4 times, 1 h for each time, and the solid-liquid ratio of 1:20. Under these extraction conditions, the content of total flavonoids in the fruit ofVernonia esculenta Hemsl. was 103.55 mg·g-1.