Dual encapsulation and sequential release of cisplatin and vitamin E from soy polysaccharides and ß-cyclodextrin bioadhesive hydrogel nanoparticles.

Chemically cross-linked hydrogel nanoparticles (HGNPs) offer enhanced properties over their physical counterparts, particularly in drug delivery and cell encapsulation. This study applied pH-thermal dual responsive bio-adhesive HGNPs for dual complexation and enhanced the controlled release and bioavailability of cisplatin (CDDP) and Vitamin E (VE) drugs. The CDDP was loaded into the HGNPs via chemical conjugation with the carboxyl groups in the HGNPs surface by soy polysaccharides (SSPS). At the same time, the host-guest interaction complexed the VE through the ß-cyclodextrin (ß-CD). The HGNPs showed a uniform HGNPs size distribution of 90.77 ± 14.77 nm and 81.425 ± 13.21 nm before and after complexation, respectively. The FTIR, XRD, XPS, and zeta potential confirmed the conjugation. The cumulative release percent of CDDP reached 98 % at pH 1.2, while <45 % was released at pH 7.4. Our HGNPs enhance the incorporation of CDDP by substituting its chlorides with carboxyl groups of the SSPS; the loading of CDDP and VE was 15 ± 0.33 and 11.32 ± 0.25 wt%, respectively. Moreover, the CDDP and VE also released slower from the HGNPs at 25 °C than at 37 °C and 42 °C. The (VE/CDDP)-loaded HGNPs exhibited longer circulation time in vivo than free CDDP and free VE suspension.

Burst Release from In Situ Forming PLGA-Based Implants: 12 Effectors and Ways of Correction.

In modern pharmaceutical technology, modified-release dosage forms, such as in situ formed implants, are gaining rapidly in popularity. These dosage forms are created based on a configurable matrix consisting of phase-sensitive polymers capable of biodegradation, a hydrophilic solvent, and the active substance suspended or dissolved in it. The most used phase-sensitive implants are based on a biocompatible and biodegradable polymer, poly(DL-lactide-co-glycolide) (PLGA). OBJECTIVE: This systematic review examines the reasons for the phenomenon of active ingredient "burst" release, which is a major drawback of PLGA-based in situ formed implants, and the likely ways to correct this phenomenon to improve the quality of in situ formed implants with a poly(DL-lactide-co-glycolide) matrix. DATA SOURCES: Actual and relevant publications in PubMed and Google Scholar databases were studied. STUDY SELECTION: The concept of the review was based on the theory developed during literature analysis of 12 effectors on burst release from in situ forming implants based on PLGA. Only those studies that sufficiently fully disclosed one or another component of the theory were included. RESULTS: The analysis resulted in development of a systematic approach called the "12 Factor System", which considers various constant and variable, endogenous and exogenous factors that can influence the nature of 'burst release' of active ingredients from PLGA polymer-based in situ formed implants. These factors include matrix porosity, polymer swelling, LA:GA ratio, PLGA end groups, polymer molecular weight, active ingredient structure, polymer concentration, polymer loading with active ingredients, polymer combination, use of co-solvents, addition of excipients, and change of dissolution conditions. This review also considered different types of kinetics of active ingredient release from in situ formed implants and the possibility of using the "burst release" phenomenon to modify the active ingredient release profile at the site of application of this dosage form.

Host-guest interaction and properties of cucurbit[8]uril with chloramphenicol.

The interaction between cucurbit[8]uril (Q[8]) and chloramphenicol (CPE) was investigated using single-crystal X-ray diffraction spectroscopy, isothermal titration calorimetry (ITC) and UV-vis, NMR and IR spectroscopy. The effects of Q[8] on the stability, in vitro release performance and antibacterial activity of CPE were also studied. The results showed that CPE and Q[8] formed a 1:1 inclusion complex (CPE@Q[8]) with an inclusion constant of 5.474 × 105 L/mol. The intervention of Q[8] did not affect the stability of CPE, but obviously reduced the release rate of CPE in artificial gastric and intestinal juice; Q[8] has a slow-release effect on CPE. The antibacterial results showed that the minimum inhibitory concentration (MIC) of CPE and CPE@Q[8] toward Escherichia coli (E. coli) was 1.5 × 10-3 and 1.0 × 10-3 mol/L, respectively, and toward Staphylococcus aureus (S. aureus), the MIC was 2.0 × 10-3 mol/L for both CPE and CPE@Q[8]. Therefore, Q[8] enhanced the inhibitory activity of CPE against E. coli.

Characterization of Cationic Modified Short Linear Glucan and Fabrication of Complex Nanoparticles with Low and High Methoxy Pectin.

In this study, we chemically modified the short linear glucan (SLG) using the 3-chloro-2-hydroxypropyl trimethylammonium chloride to introduce a positive surface charge via cationization (CSLG). We then prepared CSLG-based binary nanocomplex particles through electrostatic interactions with low and high methoxyl pectin. The two new types of binary nanocomplex were comprehensively characterized. It was found that the nanocomplex particles showed a spherical shape with the particle size of <700 nm, smooth surface, homogeneous distribution, and negative surface charge. Fourier transform infrared spectroscopy (FTIR) revealed that the driving forces to form nanocomplex were primarily electrostatic interactions and hydrogen bonding. In addition, increasing the CSLG concentration in the nanocomplex significantly enhanced both thermal stability and digestive stability. By comparing the two complex nanoparticles, the HMP-CSLG has a larger particle size and better stability under the GI condition due to the high content of the methoxy group. Additionally, the HMP-CSLG nanoparticle has a higher encapsulation efficiency and slower release rate under simulated gastrointestinal fluid for tangeretin compared with the LMP-CSLG. These results provide new insights into designing the CSLG-based nanocomplex as a potential oral delivery system for nutraceuticals or active ingredients.

In-Vitro Ibuprofen Release Monitoring Using Carbon Quantum Dots.

In this study, nitrogen-doped carbon quantum dots CQDs, synthesized from malic acid and EDTA, were encapsulated using sodium alginate. Different parameters affecting loading capacity (such as capsules' sizes, complexation solution's concentration and encapsulation method) were investigated. After that, ibuprofen (Ibu), taken as a model drug, was tagged by CQDs to form Ibu-CQDs adduct, and then encapsulated using sodium alginate. The results showed high values of loading capacity of CQDs, ibu and Ibu-CQDs capsules; 86.3%, 92% and 67%, respectively. It was proved that Ibu-CQDs release could be tracked using spectrofluorometry and UV-vis spectroscopy. The maximum release of Ibu-CQDs was 42% after 24 h. Temperature's effect on drug release was also studied and it was found that the best release was achieved at higher temperatures (40 °C), which corresponds to the illness state. Release medium's pH was also varied to simulate the pH of different parts of the gastrointestinal tract, and it was found that the best drug release can occur in the duodenum instead of the stomach. The current Ibu-CQDs capsules hold great promise for further studies in drug release and bioimaging applications.

Data of the release properties of astaxanthin-loaded zein/calcium alginate composite microparticles in fatty food simulant system at 4 °C and 25 °C.

Recently, we demonstrated the characteristics and molecular interactions of Astaxanthin (Asta), extracted from shrimp (Litopenaeus vannamei) by-products to zein/calcium alginate (CA) (named as Asta-loaded zein/CA composite microparticles). The encapsulation efficiency of Asta-zein/CA composite microparticles obtained from freeze dried, 40 °C or 50 °C oven dried was across 80% [1]. In this data, we investigted the release properties of Asta-loaded zein/CA composite microparticles in simulating fatty food system (95% ethanol solution) at 4 °C and 25 °C. At different points of time, the cumulative release percentages of Asta from the tested composite microparticles were calculated. The release kinetics of Asta from the composite microparticles was investigated using Zero order, First order, Higuchi and Rigter-Peppas models. We observed all of the tested composited microparticles displayed an initial burst effect followed by subsequent attenuating release in 4 °C and 25 °C fatty food simulant system. At 4 °C fatty food system, the Asta released from 40 °C oven dried and 50 °C oven dried composite microparticles fit best with First-order and Ritger-Peppas models, respectively. At 25 °C fatty food system, all of these tested composite microparticles fit best with Higuchi model. Our results indicate the prepared composite microparticles are expected to be used as a delivery carrier for restrained release of antioxidant Asta in fatty foods, such as in natural vegetable oils or fried foods.

Development of tilapia collagen and chitosan composite hydrogels for nanobody delivery.

Recently, injectable hydrogels have shown great potential in cell therapy and drug delivery. They can easily fill in any irregular-shaped defects and remain in desired positions after implantation using minimally invasive strategies. Here, we developed hydrogels prepared from tilapia skin collagen and chitosan (HCC). The residual mass rate of HCC was affected by the pH at the time of preparation, which was 29.1 % at pH 7 in 36 h. By comparison, the residual mass ratios of HCC at pH values of 6 and 5 were only approximately 8.4 % and 0, respectively. In addition, the stability of HCC was also affected by the concentration of these two components. HCC10 catalyzed by 10 mg mL-1 tilapia skin collagen and 10 mg mL-1 chitosan was more stable than HCC5 catalyzed by 5 mg mL-1 tilapia skin collagen and 10 mg mL-1 chitosan; therefore, we studied that ability of HCC10 to deliver two model nanobodies: 2D5 and KPU. As the concentration of nanobodies increased, the cumulative release rate of 2D5 decreased, and the release rate of KPU increased. Meanwhile, the cumulative release rate of 2D5 was the highest (68.3 %) at pH 5.5, followed by pH 6.8 (56.4 %) and 7.4 (28.4 %). However, the cumulative release rates of KPU were similar at pH 5.5 (45.1 %), 6.8 (46.5 %), and 7.4 (44.9 %). HCC is biodegradable, and can facilitate the release nanobodies; thus, HCC could be developed into an intelligent responsive tumor treatment matrix for use in cancer therapy.

A novel flunarizine hydrochloride-loaded organogel for intraocular drug delivery in situ: Design, physicochemical characteristics and inspection.

We developed a safe and efficacious drug delivery system for treatment of brain diseases. A novel in-situ gel system was prepared using soybean oil, stearic acid and N-methyl-2-pyrrolidinone (NMP) (10:1:3, v/w/v). This system had low viscosity as a sol in vitro and turned into a solid or semi-solid gel in situ after administration. The poorly water-soluble drug flunarizine hydrochloride (FNZ) was incorporated into this "organogel" system. Organogel-FNZ was characterized by light microscopy, differential scanning calorimetry (DSC) and rheology. Drug release in vitro was investigated. The initial "burst" effect did not occur in organogel-FNZ, which is different from other gels formed in situ. Pharmacokinetic studies were undertaken in rats using gel administration (14 mg kg-1), intravenous administration (5 mg kg-1) and administration using drops (14 mg kg-1). Organogel-FNZ could reduce the clearance rate and prolong the duration of action, in the plasma and brain tissues of rats. The peak serum concentration, area under the curve and absolute bioavailability of the organogel-FNZ group were higher than those of the intraocular- drops group. Organogel-FNZ is a promising drug-delivery system for treatment of brain diseases by intraocular administration.

Preparation and characterization of insulin-loaded injectable hydrogels as potential adjunctive periodontal treatment.

BACKGROUND: The application of local drugs as adjunctive periodontal treatment is a topic of rapidly increasing interest. Consequently, new discoveries are arising, a noteworthy portion of which employ hydrogels as delivery systems due to their high biocompatibility with and similarity to human tissues. In the search for new therapeutic agents capable of aiding periodontal treatment, authors became interested in a unique concept investigated by very few in vitro or in vivo studies concerning the local application of insulin. These studies concluded that insulin promotes the recovery and regeneration of damaged soft and bone tissues. OBJECTIVES: The aim of the study was an endeavor to design a linear hydrogel that is injectable into periodontal pockets, and is able to carry a small insulin load through physical bonds and provide sustained release. MATERIAL AND METHODS: The chitosan hydrogel as well as blends of polyvinyl pyrrolidone (PVP), polyvinyl alcohol (PVA) and polyethylene glycol (PEG) were prepared and characterized in terms of the hydrogel texture and injectability. Afterward, to study the insulin release kinetics, a specific amount of each formulation was loaded with insulin, and then incubated in phosphate-buffered saline (PBS). Specimens of the incubated samples were withdrawn daily to measure insulin concentrations by means of the ultraviolet (UV)-absorbance method; ultimately the cumulative release was calculated. RESULTS: Out of the 5 formulations, 4 had homogenous one-phasic texture and their insulin release profiles in vitro ranged from a few hours to about 2 weeks. The blend of 26.5 wt% PVP, 6.6 wt% PVA, 0.03 wt% calcium chloride dihydrate (CaCl2.2H2O), and 66.8 wt% water, loaded with 2 IU/g of insulin, had favorable regular sustained release, approaching 13 days. CONCLUSIONS: The composition of the hydrogel, the component ratio and the amount of loaded insulin were found to affect the release profile. A linear hydrogel of copolymerized PVP, PVA and CaCl2.2H2O can serve as a local vehicle for the sustained delivery of insulin inside periodontal pockets.

Leaching Characteristics of Heavy Metals and Plant Nutrients in the Sewage Sludge Immobilized by Composite Phosphorus-Bearing Materials.

In order to evaluate the environmental risk caused by land application of sewage sludge, leaching characteristics of heavy metals and plant nutrients in the sewage sludge immobilized by composite phosphorus-bearing materials were investigated. Their cumulative release characteristics were confirmed. Furthermore, the first-order kinetics equation, modified Elovich equation, double-constant equation, and parabolic equation were used to explore dynamic models of release. Results showed that sewage sludge addition significantly increased electricity conductivity (EC) in leachates, and the concentrations of heavy metals (Cu, Cr, Zn) and plant nutrients (N, P, K) were also obviously increased. The highest concentrations of Cu, Cr, and Zn in the leachates were all below the limit values of the fourth level in the Chinese national standard for groundwater quality (GB/T14848-2017). The immobilization of composite phosphorus-bearing materials reduced the release of Cu and Cr, while increased that of Zn. The fitting results of modified Elovich model and double-constant model were in good agreement with the leaching process of heavy metals and plant nutrients, indicating their release process in soil under simulated leaching conditions was not a simple first-order reaction, but a complex heterogeneous diffusion process controlled by multifactor.

Preparation, Characterization and Drug Release of Salicylic Acid Loaded Porous Electrospun Nanofibers.

BACKGROUND: Salicylic acid (SA), used as an important component in a lot of skin care products, has been reported widely. And because of large specific surface area, high porosity and good surfactivity, electrospun drug-loaded nanofibers have been widely used in various applications including wound dressing, tissue engineering and drug release. Particularly, the electrospun SA loaded porous nanofibers could be fabricated by regulating electrospinning (ES) parameters, and the release property of SA from nanofibers could be improved by the porous structure. Few relevant patents to the topic have been reviewed and cited. METHODS: Electrospun polylactic acid (PLA) porous nanofibers with different contents of SA were prepared successfully by modulating the ES parameters. The morphology and structure of the electrospun SA/PLA porous nanofibers were characterized by scanning electron microscopy (SEM) and flourier transformation infrared spectroscopy (FTIR). And the cumulative drug release rates of SA from SA/PLA porous nanofibers were measured using ultraviolet spectrophotometer (UV). RESULTS: The PLA concentration of 8 wt%, the SA concentrations of 4, 8, 12 wt% and the applied voltage of 15kv were selected as the optimal ES parameters. And the release percentage of low SA content was higher than that of high SA content, and the porous nanofibers had a higher cumulative release percentage of SA than the nonporous nanofibers. CONCLUSION: The release property of SA from nanofibers could be improved by the porous structure. It will provide a continuous and effective method for treating wounds.

Preparation of long-circulating dihydromyricetinliposomes and its pharmacokinetics in rats / 中草药

Objective To prepare dihydromyricetin (DMY) long-circulating liposomes and evaluate in vitro release dynamics and in vivo pharmacokinetics in rats. Methods Film-ultrasonic method was used to prepare DMY liposomes by single factor experiment and orthogonal test to optimize the formulation and preparation of DMY liposomes. The particle size and zeta potential of liposomes were determined by laser particle size analyzer. The morphological examination of liposomes was performed by using transmission electron microscopy. The liposome release in vitro was studied using dialysis method. DMY concentration in rat plasma was determined by the established LC-MS/MS method. Results The optimal prescription was 75∶20∶5 for soybean phospholipid-cholesterol-mPEG 2000-DSPE, and 1∶12 for DMY-lipid (wt/wt) with the ultrasonic time of 20 min and loading temperature of 60 ℃ in pH 5.0 PBS buffer. Under the optimized conditions, DMY liposomes was sphere with mean particle size of (117.9 ± 5.5) nm and mean zeta potential of (−2.6 ± 1.7) mV, the encapsulation efficiency and drug-loading content was (54.7 ± 3.3) % and (4.3 ± 0.2) %, respectively. The in vitro accumulative release rate of 48 h was 86% in pH 1.2 and pH 6.8 dissolve medium. Compared with free DMY, the t1/2z and AUC0-∞ of DMY liposome were increased by 2.7-fold and 1.8-fold, respectively. Conclusion Compared with free DMY, DMY liposomes released gently and slowly in vitro, eliminated slowly in vivo, and had higher bioavailability of oral administration.

Preparation of microparticles of glycyrrhetinic acid complex TOGA-X4 and in vitro release characteristics / 中草药

Objective To prepare TOGA-X4 microparticles with uniform size and good rehydration property and to obtain the stable and reliable preparation process, and evaluate the in vitro release characteristics. Methods With the average particle size, polydispersity index and rehydration as indexes, optimizing the process of antitumor active substance TOGA-X4 microparticles by stainless steel rapid film emulsification method through single factor investigation to investigate the factors influencing the size and dispersion of the drug microparticles and observe the morphology of the particles by scanning electron microscopy. With the cumulative release degree of TOGA-X4 as index, direct drug release method was adopted to determine the cumulative release rate of TOGA-X4 and the size of TOGA-X4 microparticles. The curve of in vitro drug release was fitted with different release model to estimate the in vitro release characteristics of TOGA-X4 raw powders and TOGA-X4 microparticles. Results The optimized preparation technology contained TOGA-X4 mass concentration of 5 mg/mL in oil phase, PVA mass concentration of 30 mg/mL in for aqueous phase, the ratio of oil to water was 1:1, transmembrane pressure at 0.4 MPa, sucrose aqueous solution of 50 mg/mL as freeze-drying protective agent, curing temperature at 70 ℃; Compared with other in vitro release models, the logistic equation was the fittest model to TOGA-X4 microparticles, zero order equation was the fittest model to TOGA-X4. Conclusion The preparation of microparticles by stainless steel rapid film emulsification is simple, stable and reliable, which can improve the dissolution rate of insoluble drugs and has advantages in the preparation of microparticles of poorly water-soluble drugs.

Development and Evaluation of Naproxen Sodium Gel Using Piper cubeba for Enhanced Transdermal Drug Delivery and Therapeutic Facilitation.

BACKGROUND: The absorption of drug through skin avoids many side effects of oral route like gastric irritation, nausea, systemic toxicity etc and thus improves patient compliance. Naproxen sodium (NPRS) is one of the potent NSAID agents. OBJECTIVE: The present study was aimed to develop and evaluate the gel formulation containing NPRS for transdermal drug delivery reducing the side effects and improving patient compliance. The patents on topical delivery of NSAIDS (US 9012402 B1, US 9072659 B2, US 20150258196 A1) and patents indicating use of herbal penetration enhancers (US 20100273746A1, WO 2005009510 A2, US 6004969 A) helped in selecting the drug, excipients. METHOD: Current protocol employs various extracts of Piper cubeba fruit to evaluate its role in absorption of NPRS. Various batches containing 1% NPRS and varying concentrations of synthetic permeation enhancers or the extracts were formulated in carbopol gel. Gel was evaluated for parameters like organoleptic parameters, pH, viscosity and spreadability. An ex-vivo percutaneous absorption of NPRS from gel was investigated and compared with best performing synthetic enhancer, transcutol P (TP). RESULT: The batch containing 2% n-hexane extract (NHE) of Piper cubeba showed higher permeation than TP and Chloroform (CE), Methanolic (ME) and aqueous (AE) extracts as well. It showed improved % cumulative release (85.09%) and flux (278.61µg/cm2.h), as compared to TP and other extracts. Histopathology indicated the formulation safer as compared to that with synthetic enhancer. CONCLUSION: It suggests P. cubeba as effective and safer tool for transdermal delivery and acts as therapeutic facilitator for naproxen. GC-MS analysis indicates lignans & terpenes in NHE to which this permeation enhancement activity may be attributed.

Preparation and pharmacokinetics of honokiol long-circulating liposomes / 中草药

Objective To optimize the preparation process of honokiol long-circulating liposomes (HLCL) and study the in vitro and in vivo release. Methods An orthogonal experiment was designed to optimize the composition of HLCL using entrapment efficiency as evaluation indicator. The liposome surface morphology was observed by transmission electron microscope (TEM), and the liposome release in vitro was studied by dialysis method. The concentration of honokiol in rat plasma was determined by the established LC-MS/MS method, and the differences in pharmacokinetic parameters were compared after honokiol and HLCL (20 mg/kg) were orally administered to SD male rats, respectively. Results The optimal composition of HLCL was 8:1:1 for soya phosphatidyl choline-cholesterol-mPEG2000-DSPE, and 1:10 for honokiol-liposome materials with the ultrasonic time of 12 min. Under the optimized conditions, HLCL was sphere with mean particle size of 121.5 nm and mean Zeta potential of -30.8 mV, the encapsulation efficiency and drug-loading content was 84.7% and 10.4%, respectively. In vitro release results showed that the liposomes could be gently and slowly release with the 24 h cumulative release rate at pH 1.2 and pH 6.9 dissolve medium of 80% and 71%, respectively. Based on the pharmacokinetic results, Cmax, tmax, and t1/2 were (23.29 ± 11.76) ng/mL, (0.13 ± 0.05) h and (10.59 ± 5.72) h for HLCL, and (79.34 ± 56.32) ng/mL, (0.30 ± 0.07) h and (4.44 ± 3.14) h for honokiol, respectively. There was no significant difference about the AUC0-∞ following oral administration of honokiol and HLCL at isodose honokiol (20 mg/kg). Conclusion Compared with honokiol, HLCL was released gently and slowly in vitro, absorpted rapidly and eliminated slowly in vivo.

Preparation and in vitro Release Study of Diphenidol Hydrochloride Double-layer Osmotic Pump Tablets / 中国药房

OBJECTIVE:To prepare Diphenidol hydrochloride double-layer osmotic pump tablets,and study its in vitro release characteristics. METHODS:Double-layer compressing technique and film coating technology were conducted to prepare Diphenidol hydrochloride double-layer osmotic pump tablets. The in vitro releases of it,Difenidol hydrochloride tablets in market,self-made Difenidol hydrochloride single-layer osmotic pump tablets were compared. RESULTS:The formulation was as follow as diphenidol hydrochloride 75 mg,sodium chloride 10 mg,low-molecular-weight polyoxyethylene 15 mg and right amounts of 5% PVP K30 ethanol solution. Booster layer was high-molecular-weight polyoxyethylene 60 mg,sodium chloride 20 mg,PVP K306 mg,right amounts of magnesium stearate. 12 h cumulative release(Q)of prepared double-layer osmotic pump tablets reached 80%,and the release was in line with zero-order kinetic equation. Q15 min of Difenidol hydrochloride tablets had reached 90%;Q12 h of Difenidol hy-drochloride single-layer osmotic pump tablets was only 51.14%. CONCLUSIONS:The prepared Difenidol hydrochloride dou-ble-layer osmotic pump tablets have sustained release effect,with more complete drug release within 12 h than single-layer one.

Optimizing the release process and modelling of in vitro release data of cis-dichlorodiamminoplatinum (II) encapsulated into poly(2-hydroxyethyl methacrylate) nanocarriers.

Drug encapsulated nanocarriers are vehicles to transport the drug molecules and release them at the immediate vicinity of the diseased sites. The aim of this study was to design poly (2-hydroxyethyl methacrylate) nanoparticles (PHEMANPs) as a swelling and diffusion controlled drug release system for achieving sustained release of (cis-dichlorodiamminoplatinum II) CDDP. The study undertakes designing and characterization of nanocarriers, optimization of drug encapsulation, and investigating release dynamics of the CDDP drug. PHEMANPs were prepared by suspension polymerization method followed by post loading of the CDDP onto the nanocarriers. The physicochemical and biopharmaceutical properties were evaluated by FTIR, TEM, FESEM, EDX, DLS, surface charge, water intake studies, in vitro cytotoxicity, protein adsorption and percent haemolysis. Chemical stability of the drug was assessed and in vitro release experiments were performed to optimize formulation by UV spectral analysis. The obtained cumulative release data were fitted to zero, first and Korsmeyer-Peppas kinetic models to gain insights into release kinetics and prevailing drug transport mechanisms. The successful encapsulation of CDDP was achieved in different PHEMANP formulations with maximum drug encapsulation efficiency of approx. 60% and the release kinetics was found to follow the Korsmeyer-Peppas model having non-Fickian mechanism. The results indicated that the CDDP can be formulated with a high payload of PHEMANPs which can serve as promising nanomedicine and help in achieving sustained delivery of drug for targeting tumour.

The preparation of self-microemulsifying dropping pills of paclitaxel and its drug release in vitro / 药学实践杂志

Objective The research is about optimization of preparation procedure of self-microemulsifying dropping pills of paclitaxel (PTX-SM-DP) .The drug release in vitro of PTX-SM-DP was investigated .Methods The ratio of SMEDDS and bases ,dropping distance ,temperature and speed of dripping were investigated by using the orthogonal test .The weight differ-ence of dropping pill ,hardness and roundness were evaluated to optimize the preparation conditions of PTX-SM-DP .Dissolu-tion of vitro was determined .Results The optimal preparation conditions were as follows :the ratio of SMEDDS and bases was 1∶3 ,dropping distance was 15 cm ,temperature of dripping preparation was 80 ℃ and dripping speed was 30 drops/min . Conclusion The optimized technical condition is stable and feasible .PTX-SM-DP can improve paclitaxel dissolution .

Preparation of paeoniflorin gastric floating tablets / 药学实践杂志

Objective To prepare paeoniflorin gastric floating tablets and to optimize the formulation.Methods Gastric floating tablets were prepared by wet granulation,with floating performance and in vitro cumulative release rate as evaluat indi-cators,single factor tests and orthogonal design test were adopted for the optimal formulation.Results With HPMC K4M 20% as reinforcing materials,NaHCO315% as gas agent,PVPP 7% as the release of accelerator,lactose as a filler,the ob-tained gastric floating tablet can immediately play bleaching,continued to float more than 12 hours,and the cumulative release rate was more than 90%.Conclusion The optimal formulation of paeconiflorin floating tablet has achieved a sustained and slow release request floating,the operability is good.

Preparation and in vitro release evaluation of pH-dependent colon targetting pellets of Paridis Rhizoma saponin and Astragali Radix polysaccharide / 中草药

Objective: To prepare pH-dependent Paridis Rhizoma saponin (PRS) and Astragali Radix polysaccharide (ARP) colon targeting pellets for the treatment of colon cancer and finish its in vitro release performance evaluation. Methods: The colon targeted pellets were prepared with extrusion-spheronization and air-flow coating method and the the process parameters were optimized by orthogonal design. The coating fluid prescription was investigated by single factor test. In vitro release performance evaluation of the pellets was evaluated with polyphyllin I and II as the indexes. Results: The optimum technologic parameters of extrusion spheronization equipment were as follows: the rate of extrusion was 60 r/min, the rate of spheronization was 1 200 r/min, and the time of spheronization was 5 min. The optimum coating liquid formulation of pH-dependent colon targetting pellets was 15% weight gains of Eudrugit S100, 1.5% anti-plastering aid amount of Glycerin monostearate, and 5% plasticizer amount of TEC. In vitro release test showed that cumulative release rate of berberine hydrochloride was close to 0% in artificial gastric juice after 2 h and less than 10% in artificial intestinal fluid after 4 h, but the cumulative release rate in artificial colon juice after 2 h was more than 90%. Conclusion: The preparation method can be applied to the preparation of colon targeted pellets and the pellets can achieve the targeted release in the colon.