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Licorzine granules are common preparations for children zinc deficiency. Considering the long course of treatment, the taste of licorzine granules may become a main factor affecting medication adherence. To date there have been no taste evaluation research into licorzine granules yet. In this study, both sensory evaluation and electronic tongue method were utilized to optimize licorzine granules formulations, evaluate the tastes of licorzine, excipients, optimized formulation in vivo and in vitro. As the results show, bitterness and astringency are the main unpleasant tastes generating from licorzine. Xanthan gum is the main taste-masking excipient, lowering down the bitterness and astringency of licorzine by at least one grade. Good correlation exists between the results of sensory evaluation and electronic tongue method, and an integrated combination of the two helps to obtain objective and rational research conclusions. The adult sensory evaluation study was a research-based clinical trial conducted with informed consent from all subjects in accordance with the ethical requirements of Good Clinical Practice.
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OBJECTIVE To optimize the formulation of a porcine fibrin patch （abbreviated as “DBT”）. METHODS Based on single-factor tests， with the contents of fibrinogen， thrombin and collagen before freeze-drying as the factors， with the overall desirability （OD） value of adhesion strength， holding viscosity and water absorption as response value， the formulation of DBT was optimized by Box-Behnken-response surface methodology， and the verification tests were conducted. RESULTS According to the results of the single factor tests and Box-Behnken-response surface methodology， combined with the actual production， the optimal formulation of DBT was 6.5 mg/cm2 of fibrinogen， 8.0 IU/cm2 of thrombin and 5.6 mg/mL of collagen. The average OD value of 3 validation tests was 0.726 6 （RSD＝0.58%， n＝3）， and the relative error of which with the predicted value （0.733 0） was －0.87%. CONCLUSIONS The optimal formulation of DBT is stable and feasible.
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OBJECTIVE To prepare Neuritic acid oral emulsion ，to optimize its formulation and preparation technology ，and to investigate its stability. METHODS Neuritic acid oral emulsion was prepared by mechanical method. On the basis of single factor experiment ，the appearance ，centrifugal stability ，centrifugal stability constant （Ke）and particle size of the emulsion as indexes，the formulation was optimized by orthogonal design ，taking the dosage of oleic acid ，octylphenol polyoxyethylene ether-10 and propylene glycol as factors ，the preparation technology was optimized by taking emulsification temperature ，shear time，pressure of high-pressure homogenization and cycle times of high-pressure homogenization as factors. The content of neuritic acid was determined by high performance liquid chromatography. The stability of Neuritic acid oral emulsion was investigated by high temperature test ，accelerated test and long-term test. RESULTS The optimal formulation and preparation technology were as follows：neuritic acid of 1 g，oleic acid of 5％ ，octylphenol polyoxyethylene ether- 10 of 4％ ，propylene glycol of 2％ ， emulsification temperature of 60 ℃ ，shear time of 2 min，homogenization pressure of 40 MPa and cycle times of twice. After three experiments ，the average particle size of Neuritic acid oral emulsion was 158.05 nm（RSD＝1.58％，n＝3），the average Ke was 0.39（RSD＝1.49％，n＝3），and the appearance was uniform milky white ，there was no stratification. The results of high temperature test showed that Neuritic acid oral emulsion was prone to stratification in high temperature environment ，and the content of neuritic acid increased. The results of accelerated test and long-term test showed that there was no significant change in the appearance or the content of neuritic acid when Neuritic acid oral emulsion was placed at room temperature for 6 months. CONCLUSIONS The formulation and preparation technology are stable and feasible ，and can be used for the preparation of Neuritic acid oral emulsion. Neuritic acid oral emulsion should not be placed in high temperature environment. It has good stability at room temperature for 6 months.
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Objective: India is referred as goldmine of herbal drugs but still lack of optimization of herbal drugs, which has kept us on the back foot. The rationale of the study is to prepare optimized transdermal drug delivery system of curcumin employing response surface methodology to study the collective effect of independent variables like concentration of ethyl cellulose, hydroxyl propyl methyl cellulose and dibutyl phthalate which significantly influenced characteristics like percentage elongation and in vitro drug release. Method: Twenty formulations containing varying concentrations of polymers and permeation enhancer were prepared using solvent casting technique. Result: The study revealed that the effect of dibutyl phthalate (DBP) concentration was the highest on percentage elongation (P < 0.0001), while hydroxy propyl methyl cellulose (HPMC) concentration exhibited pronounced effect on drug release (P < 0.0001) through dialysis membrane. Linear model fitted the best for curcumin release and elongation for all formulations. According to Derringer's desirability prediction tool, the composition of optimized film was found to be 242.14% of HPMC, 109.59% of ethyl cellulose (EC), and 1.03% of DBP. Under these conditions, the optimized patch exhibited a predicted value of %elongation and in vitro drug release of 94.35% and 80.0306%, respectively, which was comparable to the actual values of percent elongation and in vitro drug release i.e. 95.02% and 81.03% respectively. FTIR and thermal studies were also performed which revealed no interaction or complexation between drug and excipients. The ex vivo study performed using rat skin showed that the cumulative drug release from the optimized patch showed flux of (30.68 ± 18) µg/cm
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OBJECTIVE：To optimize the formulation of Curcumin （CUR）transethosomes（CUR-TEs）. METHODS ：The contents of CUR in CUR-TEs were determined by HPLC. CUR-TEs were prepared by injection method. Using comprehensive score of encapsulation efficiency and drug loading as index ，based on signal factor test ，Box-Behnken design-response surface method was used to optimize and validate the formulation. The property of CUR-TEs prepared by the optimal formulation was investigated. RESULTS：The optimal formulation of CUR-TEs was as follows as lecithin of 4％，CUR of 0.13％，1，2-propylene glycol of 25％，tween-80 of 1％. Results of validation test of optimal formulation showed that comprehensive score of encapsulation efficiency and drug loading of CUR-TEs was 93.04±2.16，relative error of which to predicted value （91.19）was 2.03％. The encapsulation efficiency of CUR-TEs prepared by optimal formulation was （91.17±1.35）％，and its drug loading was （0.94± 0.02）％. The particle size was （190.64±15.97）nm with polydispersity index of 0.086±0.007，and Zeta potential was （－12.74± 1.60）mV. CONCLUSIONS ：The optimized formulation of CUR-TEs is stable ，feasible and repeatable ，with good stability.
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OBJECTIVE: To optimize the formulation of citalopram hydrobromide (CTH ) thermosensitive nasal gel and further evaluate its in vitro properties. METHODS: With gelling temperature and gelling time as evaluating indexes, central composite design-response surface and single factor experimental design method were used to optimize the formulation of CTH thermosensitive nasal gel by using poloxamer 407(F127) and carbomer 940 (CP940) as gel materials. Meanwhile, nasal mucosa permeation enhancer for CTH was then sieved by using Franz diffusion cell and ex vivo sheep nasal mucosa as experimental model. Finally, CTH thermosensitive nasal gel was prepared with cold method and then its in vitro properties was evaluated. In vitro cumulative erosion and cumulative release rate of the drug thermosensitive nasal gel were investigated by membrane-free dissolution method and dialysis membrane method, respectively. Moreover, the effect of temperature and pH on the viscosity of the drug nasal gel formulation was also evaluated. RESULTS: The optimal formulation of the thermosensitive nasal gel consisted of CTH 8.0%, F127 20.27%, CP940 0.17%, DM-β-CD 3.0%, ethylparaben 0.05% and distilled water. The gelling temperature, gelling time and pH of the drug thermosensitive nasal gel were found to be about 32.5 ℃,42 s and 5.0, respectively. The in vitro cumulative erosion and cumulative release percentage were both greater than 90% in 55 min and furthermore there was good linear correlation between these two parameters (r=0.998 6). Additionally, in vitro cumulative release of the drug from the gel formulation was determined to be 92% within 8 h, which conformed to Higuchi kinetic equation. Furthermore, the viscosity of the drug nasal gel was influenced by temperature as well as pH in different extent. CONCLUSION: The optimized formulation of the CTH thermosensitive nasal gel with central composite design-response surface method and single factor design method shows suitable gelling temperature, gelling time, pH value for nasal preparation and obvious in vitro drug sustained release characteristics.
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OBJECTIVE：To optimize the formul ation of Polygala japonica cream，and to evaluate the quality of prepared cream. METHODS ：With centrifugal stability ，heat resistance stability and viscosity as evaluation indexes ，the weight coefficient was determined by analytic hierarchy process （AHP），criteria importance through intercriteria correlation （CRITIC）method and mixed weighted AHP-CRITIC ，and the comprehensive score was calculated. The amount of octadecyl alcohol ，hexadecanol and mixed emulsifier （polysorbate 60 mixed with glycerin monostearate at the mass ratio of 2.82）in the formulation of P. japonica cream were screened by central composite design-response surface methodology. The optimized formulation was validated. P. japonica cream prepared by the optimal preparation was evaluated in terms of apperance ，particle，pH，stability and rheological characteristics. RESULTS ：The weight coefficients of centrifugal stability ，heat resistance stability and viscosity were 0.428 5， 0.415 6 and 0.155 9 respectively，according to the mixed weighted AHP-CRITIC. The optimal formulations were 1.96 g of hexadecyl alcohol ，5.17 g of octadecyl alcohol ，2.48 g of mixed emulsifier ，1.83 g of polysorbate 60，0.65 g of glyceride monostearate，1 g of benzyl alcohol ，5 g of propylene glycol ，6 g of isopropyl myristate and 5 g of P. japonica extract，and then added water to 100 g. Prepared cream was a light yellow fluid paste with particle size of 0.5-2.5 μm and pH value of 6.5；the results of centrifugal test ，heat resistance test and cold resistance stability test showed that the cream had no oil-water separation or thickened paste. The prepared cream was shear-thinning non-Newtonian fluid. CONCLUSIONS ：P. japonica cream is prepared successfully，which shows good apperance ，particle，acidity and stability.
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OBJECTIVE：To prepare GGPFV-modified Daunorubicin/dioscin liposomes ，and to optimize their formulation and to preliminarily evaluate their cytotoxicity to breast cancer cells in vitro . METHODS ：Daunorubicin and diosgenin were wrapped by thin film dispersion method and ammonium sulfate hydration method ；the surface was modified with DSPE-PEG2000-GGPFV to prepare GGPFV-modified Daunorubicin/dioscin liposomes. Taking encapsulation rate as index ，Box-Behnken response surface methodology was used to optimize the film hydration volume ，cholesterol amount and daunorubicin amount in the formulation. The entrapment efficiency of 3 batches of liposomes prepared according to the optimal formulation was determined. The effects of Daunorubicin/dioscin liposomes ，GGPFV-modified Daunorubicin/dioscin liposomes and blank liposomes on the survival rate of human breast cancer MDA-MB- 435S cells were compared. RESULTS ：The optimal formulation was as film hydration volume of 5 mL，cholesterol of 4 mg，yolk lecithin of 22 mg，daunorubicin of 0.55 mg，dioscin of 0.85 mg，DSPE-PEG2000 of 3.5 mg， DSPE-PEG2000-GGPFV of 2 mg. The encapsulation rate of daunorubicin was （96.21±1.54）％ and that of dioscin was （95.39± 2.48）％ in the 3 batches of liposomes prepared. The in vitro cytotoxicity tests showed that the inhibition effect of GGPFV-modified Daunorubicin/dioscin liposome on MDA-MB-435S cells was significantly stronger than that of Daunorubicin/dioscin liposome （P＜ 0.05）. There was no cytotoxicity in the membrane. CONCLUSIONS ：GGPFV-modified Daunorubicin/dioscin liposomes are successfully prepared ，and its inhibitory effect on human breast cancer MDA-MB- 435S cells in vitro was significantly enhanced.
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Objective: To prepare carboxymethyl Bletilla striata polysaccharide-chitosan@curcumin (CM-BSP) polyelectrolyte complex films, optimize their preparation technology, and evaluate its quality. Methods: CM-BSP was synthesized, then CM-BSP and CS formed water-insoluble complex by electrostatic bonding, the Cur-loaded polyelectrolyte complex films were prepared by a volatilization of solvent method. The formulation and preparation technology were optimized using an orthogonal design method and the morphology and structure were observed by scanning electron microscopy and fourier transform microscopic infrared spectroscopy. Results: The optimal prescription was of CM-BSP 117 mg, CS 233 mg, glycerol 25%, Cur 20 mg. The mean thickness of Cur-loaded polyelectrolyte complex films was (74.0 ± 2.0) μm, drug loading capacities was 95.41%, and in vitro release rate was 93.78%. Conclusion: The obtained polyelectrolyte complex films displayed an smooth exterior inspection, uniform distribution, good drug loading capacities and in vitro release rate.
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OBJECTIVE：To study the prepar ation technology of gastric floating tablets of Schisandra chinensis total lignans （SCTL），and evaluate the quality of prepared tablets. METHODS ：Based on single factor test ，the orthogonal experiment was conducted to optimize the formulation of SCTL gastric floating tablets with the contents of hydroxypropylmethylcellulose （HPMC） K15M，NaHCO3 and microcrystalline cellulose as the factors ，using starting time ，holding time and cumulative release rate of gastric floating tablets as evaluation indexes. The properties ，weight difference ，floatability and accumulative release rate of the prepared SCTL gastric floating tablets were determined. The gastric floating tablets were qualitatively identified by TLC ，and the contents of schisandrin A and total lignans were determined by HPLC and UV spectrophotometry. RESULTS ：The optimal formulation of SCTL gastric floating tablets was made up of 23％ SCTL extract ，20％ HPMC K 15M，40％ microcrystalline cellulose，15％ sodium bicarbonate ，1％ octadecyl alcohol and 1％ polyvinylpyrrolidone. The results of detection of this preparation were in line with the related provisions of “0101 tablet”stated in 2015 edition of Chinese Pharmacopoeia （part Ⅳ）. TLC indicated that the chromatogram of the test sample showed the main spots of same color as the corresponding positions of the chromatogram of schizandrol A control ，Schisandra chinensis reference substance and raw material ，while the negative control has no interference. Content determination results shows that the average content of schizandrol A and total lignans in SCTL gastric floating tablets is 3.187，19.617 mg. It was preliminarily formulated that the content limitation of schizandrol A in one tablet should not be less than 2.50 mg，and the content of total lignans （calculated by schizandrol A ）should not be less than 15.50 mg. CONCLUSIONS：The preparation technology of SCTL gastric floating tablets is stable ，feasible and controllable in quality.
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OBJECTIVE：To prepare Imperatorin ultradeformable liposomes gel （IMP-UDLs-Gel），and to evaluate its quality. METHODS：Based on single factor test ，using 12 h accumulative penetration amount （Q12h）as evaluation index ，the proportion of carbomer 940，glycerol and propyl glycol in formulation of IMP-UDLs-Gel were investigated by orthogonal test. The optimal formulation was screened. The quality of IMP-UDLs-Gel prepared with the optimal formulation was evaluated. RESULTS ：The optimal formulation of IMP-UDLs-Gel included carbomer 940 proportion of 1％，glycerol proportion of 15％ and propyl glycol proportion of 10％. Q12 h of IMP-UDLs-Gel was （11.543±0.241）μg/cm2；the appearance was milky white and translucent ；the particle size was （93.13±1.68）nm，PDI was 0.268±0.012，Zeta potential was （－24.96±1.99）mV；pH was 7.32±0.03； viscosity was （45.37±1.27）g·s；steady flow was （0.727±0.002）μg·h/cm2，lag time was （4.358±0.175）h，apparent permeability coefficient was 1.392×10－3 cm/h，and it has good physical and optical stability. CONCLUSIONS ：The preparation method is stable and feasible ，and the prepared IMP-UDLs-Gel has good adhesion ，stability and transdermal property.
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Objective To prepare a wound dressing using nitrocellulose as a membrane and optimize its formulation. Methods Partial analysis was performed on commercial available products. The wound dressings were prepared by using nitrocellulose as a film-forming material, benzyl alcohol as a bacteriostatic agent, castor oil as a plasticizer, isopropyl palmitate as a skin emollient, camphor as a fragrance, and isopropyl alcohol, ethyl acetate and butyl acetate as volatile solvent. The tensile strength, breakpoint elongation percentage, breathability and waterproof performance were tested and evaluated. Results The film-forming performance of the prepared liquid wound dressing was good. The final use amount of nitrocellulose was determined to be 6%. The use amount of plasticizer castor oil was determined to be 4%. Conclusion The prepared liquid wound dressing has good film-forming property, good mechanical property, good waterproof and certain breathability.
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OBJECTIVE：To prepar e Breviscapine gastric adhesive tablets ，to optimize the formulation and to evaluate the quality. METHODS ：HPMC K 100M and carbomer 934P were used as bioadhesives and skeleton materials ，and lactose was used as filler，and magnesium stearate was used as glidant and lubricant to prepare Breviscapine gastric adhesive tablets by direct powder pressing method. The comprehensive scores of scores of accumulative release rate of Breviscapine gastric adhesive tablets in pH 6.8 PBS at 2，6，12 h（Q2 h，Q6 h，Q12 h，with scutellarin meter ，by HPLC method ）and in vitro adhesion force of gastric tissue were evaluated by weighting method. Taking this scores as indexes，L9（34）orthogonal test design was used to optimize the amount of HPMC K 100M，carbomer 934P and lactose in Breviscapine gastric adhesive tablets and validation tests were conducted. The properties，identification，weight difference ，fragility，release and the content of scutellarin of the gastric adhesive tablets were determined. RESULTS ：The optimal prescription of Breviscapine gastric adhesive tablets were 42％ breviscapine，10％ HPMC K100M，3％ carbomer 934P and 45％ lactose. The verification test results show that the Q2 h，Q6 h，Q12 h of 3 batches of Breviscapine gastric adhesive tablets were 20.36％，48.55％，and 87.00％ ；the average in vitro adhesion force of gastric tissue was 31.36 g/cm2；the average comprehensive score was 70.23（RSD＝1.84％，n＝3）. The gastric adhesive tablets were light yellow，tasteless or slightly salty ；the peak time was consistent with that of scutellarin control ；its weight difference were ±6％， the fragility was 0.54％，and the Q12 h was 83.51％（RSD＝2.14％，n＝6）. The content of scutellarin was 288.47 mg/g（RSD＝ 0.70％，n＝3）. CONCLUSIONS ：Breviscapine gastric adhesive tablets is prepared successfully ，and its quality evaluation conforms to the requirements of Chinese Pharmacopoeia （2015 edition）.
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OBJECTIVE： To optimize the formulation of Diosmin gel and to investigate its in vitro release property. METHODS： Diosmin gel were prepared by using Carbomer 940 as matrix. Using accumulative release rate as index， with the amount of Carbomer 940， ethanol， acetone and pH as factors， L9（34） orthogonal test was conducted. The formulation of Diosmin gel was optimized and validated. Using Diosmin ointment as reference， dialysis bag diffusion method was used to investigate in vitro release property of Diosmin gel prepared by optimal formulation. RESULTS： The optimal formulation of Diosmin gel included Carbomer 940 1.5 g， ethanol 15 mL， glycerol 8 g， pH 6. The gel prepared with optimal formulation was sticky brown-yellow semi solid， and had good coating and spreading properties. The average accumulative release rate （2 h） was （12.67±0.12）％. Results of drug release test showed that Diosmin gel released rapidly within 12 h， then gradually slowed down. The accumulative release rates were （71.93±0.42）％ （12 h） and （80.47±0.54）％ （24 h）， drug release of which were in line with Higuchi equation. Diosmin ointment was released slowly. The accumulative release rates were （41.74±0.18）％ （12 h） and （62.63±0.59）％ （24 h）. Drug release of it were in line with first-order equation. CONCLUSIONS： The formulation of Diosmin gel is optimized successfully. Prepared Diosmin gel has good drug release property.
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Objective: The preparation process of curcumin-loaded TPGS/F127/P123 mixed micelles was optimized with uniform design method to improve the poor solubility of curcumin in water, aiming to increase entrapment efficiency (EE), drug-loading (DL), and reduce the precipitated drug (PD). Methods: Curcumin-loaded TPGS/F127/P123 mixed micelles were prepared by thin-film hydration method with modification. Before using the uniform design, a number of preliminary experiments were conducted to identify the controlled factors such as the amount of curcumin, the dosage of TPGS, and the ratio of F127/P123. The formulation was operated by uniform design of three factors and seven levels, and its results were fitted by polynomial linear equation, the response surface, and the contour line in order to choose and verify the optimal preparation process. Results: In the optimum formulation, the dosage of curcumin was 14.0 mg, TPGS 150.0 mg, and the ratio of F127/P123 was 68: 32. The solubility of optimum formulation was (3.47 ± 0.14) mg/mL, EE (87.15 ± 4.39)%, DL (4.70 ± 0.17)%, and PD (0.33 ± 0.12)% in 48 h. Conclusion: The solubility of curcumin in TPGS/F127/P123 mixed micelles was improved after the optimization of the uniform design method, and EE and DL were also improved.
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Objective To prepare reactive oxygen species (ROS)-responsive Bletilla striata polysaccharide (Oxi-BSP) micelles, optimize their preparation technnology, and evaluate its in vitro characterizations. Methods Oxi-BSP was synthesized, then curcumin (Cur)-loaded micelles were prepared by a dialysis method. The formulation and preparation technology was optimized using an orthogonal design method. The morphology was observed by transmission electron microscope, while the particle size, particle distribution, and zeta potential were determined by laser particle size analyzer. Hydrogen peroxide was used to simulate the ROS environment and then the change of micellar morphology was observed. Results The Cur-loaded micelles were spherical with homogeneous distribution, the mean size was (225.33 ± 2.97) nm, the zeta potential was (-16.80 ± 0.37) mV, the encapsulation efficiencies was (85.75 ± 0.87)%, and drug loading capacities was (20.21 ± 0.44)%. And the micelles were responsive to ROS stimuli. Conclusion The obtained micelles display an uniform particle size distribution with moderate drug encapsulation efficiencies and drug loading capacities.
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OBJECTIVE:To optimize the formulation of Roxatidine acetate hydrochloride(ROX)sustained-release tablets. METHODS:ROX sustained-release tablets were prepared by direct powder compression method. Central composite design-response surface methodology was used to optimize the formulation with composite index of 1,4,8 h in vitro accumulative release rate as index,using mass ratio of lactose/microcrystalline cellulose(MCC)(m/m),ethyl cellulose(EC)amount and HPMC amount as factors. Validation test was also conducted. RESULTS:The optimal formulation was as follows as ROX 75 mg,lactose 45 mg, MCC 91 mg,EC 65 mg,HPMC 124 mg,micropowder silica gel 2 mg. 1,4,8 h in vitro accumulative release rates of prepared sustained-release tablets were(30.7 ± 0.5)%,(65.8 ± 0.7)%,(89.4 ± 0.6)%,respectively. Related errors of them to predicted value were 0.6%,0.8%,1.2%,respectively. CONCLUSIONS:ROX sustained-release tablets are prepared successfully,and sustained-release effect is consisted with the expected effect.
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OBJECTIVE:To prepare Bevacizumab(BEV)multivesicular liposomes(BEV-MVLs)with sustained-effect,and to study their in vitro release characteristics. METHODS:BEV-MVLs were prepared by double emulsion method. Box-Behnken design-response surface methodology was used to optimize the prescription with the concentration of glycerol trioleate(TO)in organic phase,ratio of 1,2-dioleoyl-sn-glycero-3-phosphocholine(DOPC)-cholesterol(CH)(mol/mol),the concentration of L-lysine in external water phase as factors,using encapsulation rate as index. The morphology of BEV-MVLs was observed by inverted fluorescence microscope and SEM;particle size was determined by laser particle size analyzer;the BEV content was determined by HPLC and calculate the encapsulation rate and in vitro accumulative release rate.RESULTS:The optimized prescription was as follows as TO of 2.72 mmol/L in organic phase,DOPC-CH ratio of 0.67(mol/mol)and L-lysine of 40 mmol/L in external water phase. The encapsulation rate of BEV-MVLs was(80.65±4.42)%(n=3),and relative error of it to predicted value was 2.54%. The liposomes were spherical in appearance shape and uniform in size,and they were typical non-concentric vesicle structure with average particle size of 16.80 μm. 30 d in vitro accumulative release rate was about 92%. CONCLUSIONS:Prepared BEV-MVLs show sustained-effect,and their encapsulation rate reaches the expected effect.
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OBJECTIVE:To optimize the formulation of Phencynonate hydrochloride transdermal patch. METHODS:Phencynonate hydrochloride transdermal patch was prepared by solvent evaporation method. Using 48 h accumulative transdermal volume as index,single factor test and Box-Behnken design-response surface methodology were used to optimize drug dosage,the amount of transdermal enhancers azone and pressure-sensitive adhesive,and evaluate the appearance,adhesion of the formulation prepared by the best prescription. RESULTS:The optimized formulation was as follows as 263 mg drug dosage,165 mg azone, 1.94 g pressure-sensitive adhesive and 1.6 g methanol. 48 h accumulative transdermal volume of prepared patch was(119.48 ± 2.95)μ g/cm2(n=5),related error of which to predicted value was 2.48%. The prepared patch showed smooth surface and incision,good adhesiveness. CONCLUSIONS:Phencynonate hydrochloride transdermal patch is prepared successfully,its accumulative transdermal volume is in agreement with predicted standard.
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OBJECTIVE: To prepare Wheat germ agglutinin (WGA) modified vinorelbine (VRB) cationic liposomes (WGA-VRB cationic liposomes), and to optimize the formulation and conduct cytotoxicity test.METHODS: Thin-film diffusion and ammonium sulfate gradient method were used to prepare WGA-VRB cationic liposomes using phospholipid and cholesterol as excipient, 3β-[N-(N' -N' -dimethyl aminoethane) -carbamoyl] cholesterol hydrochloride (DC-Chol) as cationic material, distearoyl phosphatidylethanolamine-polyethylene glycol 2000 (DSPE-PEG2000) as long cycle chain. Using encapsulation rate as index, central composite design-response surface methodology was used to optimize the amount of DC-Chol, cholesterol and VRB. The contents of VRB in VRB liposomes and WGA-VRB cationic liposomes were determined. The effects of them and blank cationic liposomes on survival rates of human breast cancer cell MCF-7 and human non-small cell lung cancer cells A549 were compared. RESULTS: The optimal formulation of 5 mL WGA-VRB cationic liposomes was as follows as phospholipid 22 mg, cholesterol 12 mg, DC-Chol 8 mg, VRB 0. 5 mg. Encapsulation rate of the liposomes was (92. 24 ± 1. 21)％ (n=3), relative error of which to predicted value was 5. 3％. The contents of VRB in VRB liposomes and WGA-VRB cationic liposomes were (96. 01 ± 3. 26), (93. 39 ± 1. 59) μg/mL(n=3). Compared with blank cationic liposomes and VRB liposomes, WGA-VRB cationic liposomes could significantly reduce survival rate of MCF-7 and A549. CONCLUSIONS: WGA-VRB cationic liposomes are prepared successfully. Inhibitory effect of WGA-VRB cationic liposomes on MCF-7 and A549 cell survival is stronger than that of VRB liposomes.