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  • 1.

    【2hr】A Novel Topical Targeting System of Caffeine Microemulsion for Inhibiting UVB-Induced Skin Tumor: Characterization, Optimization, and Evaluation

    包量

    机译 咖啡因微乳液抑制UVB诱导的皮肤肿瘤的新型主题靶向系统：表征，优化和评估。
    摘要：The purpose of the present study was to develop an optimal microemulsion (ME) formulation as topical nanocarrier of caffeine (CAF) to enhance CAF skin retention and subsequently improve its therapeutic effect on UVB-induced skin carcinogenesis. The pseudo-ternary phase diagram was developed composing of Labrafil M 1944 CS as oil phase, Cremophor EL as surfactant, tetraglycol as cosurfactant, and water. Four ME formulations at water content of 50, 60, 70, and 80% were prepared along the water dilution line of oil to surfactant ratio of 1:3 and characterized in terms of morphology, droplet size, and electric conductivity. A gel at the same drug loads (1%, w/w) was used as control. Ex vivo skin permeation studies were conducted for ME optimization. The optimized formulation (ME4) was composed of 5% (w/w) Labrafil M 1944 CS, 15% (w/w) Smix (2/1, Cremophor EL and tetraglycol), and 80% (w/w) aqueous phase. The skin location amount of CAF from ME4 was nearly 3-fold higher than control (P < 0.05) with improved permeated amount through the skin. The skin targeting localization of hydrophilic substance from ME4 was further visualized through fluorescent-labeled ME by a confocal laser scanning microscope. In pharmacodynamics studies, CAF-loaded ME4 was superior in terms of increasing apoptotic sunburn cells (P < 0.05) as compared with control. Overall results suggested that the ME4 might be a promising vehicle for the topical delivery of CAF.
  • 2.

    【2hr】The Stabilization of Amorphous Zopiclone in an Amorphous Solid Dispersion

    包量

    机译 非晶态固体分散体中非晶态佐匹克隆的稳定性
    摘要：Zopiclone is a poorly soluble psychotherapeutic agent. The aim of this study was to prepare and characterize an amorphous form of zopiclone as well as the characterization and performance of a stable amorphous solid dispersion. The amorphous form was prepared by the well-known method of quench-cooling of the melt. The solid dispersion was prepared by a solvent evaporation method of zopiclone, polyvinylpyrrolidone-25 (PVP-25), and methanol, followed by freeze-drying. The physico-chemical properties and stability of amorphous zopiclone and the solid dispersion was studied using differential scanning calorimetry (DSC), infrared spectroscopy (FT-IR), thermogravimetric analysis (TGA), scanning electron microscopy (SEM), hot-stage microscopy (HSM), X-ray diffractometry (XRD), solubility, and dissolution studies. The zopiclone amorphous solid-state form was determined to be a fragile glass; it was concluded that the stability of the amorphous form is influenced by both temperature and water. Exposure of amorphous zopiclone to moisture results in rapid transformation of the amorphous form to the crystalline dihydrated form. In comparison, the amorphous solid dispersion proved to be more stable with increased aqueous solubility.
  • 3.

    【2hr】Electrospinning of Cross-Linked Magnetic Chitosan Nanofibers for Protein Release

    包量

    机译 交联磁性壳聚糖纳米纤维的静电纺丝用于蛋白质释放
    摘要：A poly(vinylalcohol) (PVA) electrospun/magnetic/chitosan nanocomposite fibrous cross-linked network was fabricated using in situ cross-linking electrospinning technique and used for bovine serum albumin (BSA) loading and release applications. Sodium tripolyphosphate (TPP) and glutaraldehyde (GA) were used as cross-linkers which modified magnetic-Fe3O4 chitosan as Fe3O4/CS/TPP and Fe3O4/CS/GA, respectively. BSA was used as a model protein drugs which was encapsulated to form Fe3O4/CS/TPP/BSA and Fe3O4/CS/GA/BSA nanoparticles. The composites were electrospun with PVA to form nanofibers. Nanofibers were characterized by field emission scanning electron microscopy (FESEM) and Fourier transform infrared spectroscopy (FTIR). The characterization results suggest that Fe3O4 nanoparticles with average size of 45 nm were successfully bound on the surface of chitosan. The cross-linked nanofibers were found to contain uniformly dispersed Fe3O4 nanoparticles. The size and morphology of the nanofibers network was controlled by varying the cross-linker type. FTIR data show that these two polymers have intermolecular interactions. The sample with TPP cross-linker showed an enhancement of the controlled release properties of BSA during 30-h experimental investigation.

    Graphical Abstractᅟ

  • 4.

    【2hr】Influence of Process and Formulation Parameters on Dissolution and Stability Characteristics of Kollidon® VA 64 Hot-Melt Extrudates

    包量

    机译 工艺和配方参数对Kollidon®VA 64热熔挤出物溶解度和稳定性的影响
    摘要：The objective of the present study was to investigate the effects of processing variables and formulation factors on the characteristics of hot-melt extrudates containing a copolymer (Kollidon® VA 64). Nifedipine was used as a model drug in all of the extrudates. Differential scanning calorimetry (DSC) was utilized on the physical mixtures and melts of varying drug–polymer concentrations to study their miscibility. The drug–polymer binary mixtures were studied for powder flow, drug release, and physical and chemical stabilities. The effects of moisture absorption on the content uniformity of the extrudates were also studied. Processing the materials at lower barrel temperatures (115–135°C) and higher screw speeds (50–100 rpm) exhibited higher post-processing drug content (~99–100%). DSC and X-ray diffraction studies confirmed that melt extrusion of drug–polymer mixtures led to the formation of solid dispersions. Interestingly, the extrusion process also enhanced the powder flow characteristics, which occurred irrespective of the drug load (up to 40% w/w). Moreover, the content uniformity of the extrudates, unlike the physical mixtures, was not sensitive to the amount of moisture absorbed. The extrusion conditions did not influence drug release from the extrudates; however, release was greatly affected by the drug loading. Additionally, the drug release from the physical mixture of nifedipine–Kollidon® VA 64 was significantly different when compared to the corresponding extrudates (f2 = 36.70). The extrudates exhibited both physical and chemical stabilities throughout the period of study. Overall, hot-melt extrusion technology in combination with Kollidon® VA 64 produced extrudates capable of higher drug loading, with enhanced flow characteristics, and excellent stability.
  • 5.

    【2hr】A Non-invasive Method for the Determination of Liquid Injectables by Raman Spectroscopy

    包量

    机译 拉曼光谱法测定液体注射剂的非侵入性方法
    摘要：Drug safety has become a very important subject, and more countries have joined in the fight against counterfeit drugs. This study demonstrated a non-invasive Raman spectroscopy method that could be utilized for screening liquid injectable drugs for spurious/falsely-labeled/falsified/counterfeit medical products (SFFCs). Two problems were solved to remove the blocks in identification and quantitation: one problem was the weak API signal extraction from the non-invasive Raman spectra and the other was the problem of Raman absolute measurement. Principal component analysis (PCA) and classical least square (CLS) algorithms were performed to establish the models. Water was chosen as the “internal standard” to normalize the spectra to solve the problem of Raman absolute measurement. The results showed that the 11 positive samples and 66 negative samples were all well identified with a threshold of 0.95. One of the positive samples contained the excipient propylene glycol, which was identified successfully at the same time. The accuracy of quantitative results was approximately 5% for doxofylline liquid injectables and about 10% for the low-concentration and big glass bottle-containers of Levofloxacin Lactate and Sodium Chloride Injections as compared to the results using an HPLC method, this is satisfactory for fast screening of SFFCs. In conclusion, with the development of a database of identification and quantitation models, this method may determine liquid injectable drugs in a fast and non-invasive way and become one of the most powerful weapons against SFFCs.

    Graphical Abstractᅟ

  • 6.

    【2hr】Sublingual Diffusion of Epinephrine Microcrystals from Rapidly Disintegrating Tablets for the Potential First-Aid Treatment of Anaphylaxis: In Vitro and Ex Vivo Study

    包量

    机译 肾上腺素微晶从快速崩解片的舌下扩散对过敏反应的潜在急救方法：体内和体外研究
    摘要：For the first-aid treatment of anaphylaxis, epinephrine (Epi) 0.3 mg intramuscular (IM) injection in the thigh is the drug of choice. Epi auto-injectors are widely recommended for anaphylaxis treatment in community settings but not necessarily carried or used as prescribed when anaphylaxis occurs. We therefore developed rapidly disintegrating sublingual tablets (RDSTs) as an alternative noninvasive dosage form. Our objective in this study was to evaluate the effect of reducing Epi particle size on its in vitro and ex vivo diffusion, with the goal of enhancing Epi sublingual absorption from Epi RDSTs. Epi particle size was reduced by top-bottom technique using a microfluidizer for one pass at 30,000 Psi. The micronized Epi crystals (Epi-MC) were characterized using Zetasizer, Fourier transform infrared (FT-IR), differential scanning calorimetry (DSC), and scanning electron microscopy (SEM). Epi RDSTs were formulated and manufactured using our previously developed method. In vitro and ex vivo diffusion of Epi 10, 20, and 40 mg RDSTs and Epi-MC 10 and 20 mg RDSTs (n = 4) were evaluated using Franz cells. Epi 10 mg solution was used as a control. Mean (±standard deviation (SD)) Epi particle size was successfully reduced from 131.8 ± 10.5 to 2.5 ± 0.4 μm. Cumulative Epi diffused and influx from 40 mg Epi RDSTs and 20 mg Epi-MC RDSTs were not significantly different from each other in vitro and ex vivo (p > 0.05). Also, Epi permeability from 20 mg Epi-MC RDSTs was significantly higher than from the rest (p < 0.05). Epi-MC RDSTs improved Epi diffusion twofold and might have the potential to reduce the Epi dose needed in RDSTs by 50%.
  • 7.

    【2hr】Masking the Bitter Taste of Injectable Lidocaine HCl Formulation for Dental Procedures

    包量

    机译 掩盖用于牙科手术的可注射盐酸利多卡因制剂的苦味
    摘要：Several attempts have been made to mask the bitter taste of oral formulations, but none have been made for injectable formulations. This study aims to mask the bitter taste of dental lidocaine HCl (LID) injection using hydroxypropyl-β-cyclodextrin (HP-β-CD) and sodium saccharin. Inclusion complexes of LID and HP-β-CD were prepared by the solution method in 1:1 and 1:2 M ratios. Inclusion complexes in solution were studied using phase solubility in phosphate buffer solutions (pH 8, 9, and 10). Freeze-dried inclusion complexes were characterized using differential scanning calorimetry (DSC), X-ray, Fourier transform infrared (FT-IR), nuclear magnetic resonance (NMR), scanning electron microscopy (SEM), and in vitro release. Injectable formulations were prepared using inclusion complexes and characterized for stability and for taste using an Alpha MOS ASTREE electronic tongue (ETongue). The association constants of HP-β-CD with lidocaine-free base and its ionized form were found to be 26.23 ± 0.00025 and 0.8694 ± 0.00045 M−1, respectively. Characterization studies confirmed the formation of stable inclusion complexes of LID and HP-β-CD. Injectable formulations were found to be stable for up to 6 months at 4°C, 25°C, and 40°C. The taste evaluation study indicated that HP-β-CD (1:1 and 1:2 M ratios) significantly improved the bitter taste of LID injectable formulation. In conclusion, inclusion complex in the 1:1 M ratio with 0.09% sodium saccharin was considered to be optimum in masking the bitter taste of LID.
  • 8.

    【2hr】The Improvement of the Dissolution Rate of Ziprasidone Free Base from Solid Oral Formulations

    包量

    机译 固体口服制剂提高齐普拉西酮游离碱的溶解速率
    摘要：This work aims at increasing solubility and dissolution rate of ziprasidone free base—Biopharmaceutics Classifaction System (BCS) class II compound. The authors describe a practical approach to amorphization and highlight problems that may occur during the development of formulations containing amorphous ziprasidone, which was obtained by grinding in high-energy planetary ball mills or cryogenic mills. The release of ziprasidone free base from the developed formulations was compared to the reference drug product containing crystalline ziprasidone hydrochloride—Zeldox® hard gelatin capsules. All preparations were investigated using compendial tests (USP apparatuses II and IV) as well as novel, biorelevant dissolution tests. The novel test methods simulate additional elements of mechanical and hydrodynamic stresses, which have an impact on solid oral dosage forms, especially during gastric emptying. This step may prove to be particularly important for many formulations of BCS class II drugs that are often characterized by narrow absorption window, such as ziprasidone. The dissolution rate of the developed ziprasidone free base preparations was found to be comparable or even higher than in the case of the reference formulation containing ziprasidone hydrochloride, whose water solubility is about 400 times higher than its free base.
  • 9.

    【2hr】Effervescence Assisted Fusion Technique to Enhance the Solubility of Drugs

    包量

    机译 泡腾辅助融合技术可提高药物的溶解度
    摘要：The solubility of five poorly soluble drugs was enhanced by using an effervescence assisted solid dispersion (EASD) technique. EASDs were prepared by using modified fusion method. Drug and hydrophilic carrier were melted, and in this molten mixture, effervescence was generated by adding effervescence couple comprising organic acid (citric acid) and carbonic base (sodium bicarbonate). Solubility of drug powders, solid dispersions, and EASDs was determined at 25°C using shake flask method. Atorvastatin calcium, cefuroxime axetil, clotrimazole, ketoconazole, and metronidazole benzoate were estimated using a spectrophotometer at 246, 280, 260, 230, and 232 nm (λmax), respectively. Solubility of atorvastatin calcium (from 100 to 345 μg/ml), cefuroxime axetil (from 441 to 1948 μg/ml), clotrimazole (from 63 to 677 μg/ml), ketoconazole (from 16 to 500 μg/ml), and metronidazole benzoate (from 112 to 208 μg/ml) in EASDs was enhanced by 3.45-, 4.4-, 10.7-, 31.2-, and 1.8-fold, respectively. Scanning electron micrographs of drug powder, solid dispersion, and EASDs were compared. Scanning electron micrographs of EASDs showed a uniform distribution of drug particles in the carrier matrix. Morphology (size and shape) of cefuroxime axetil particles was altered in solid dispersion as well as in EASD. EASDs showed better solubility enhancement than conventional solid dispersions. The present technique is better suitable for drugs having a low melting point or melt without charring. Effervescence assisted fusion technique of preparing solid dispersions can be employed for enhancing solubility, dissolution, and bioavailability of poorly soluble drugs.
  • 10.

    【2hr】Synthesis of Mono-PEGylated Growth Hormone Releasing Peptide-2 and Investigation of its Biological Activity

    包量

    机译 单聚乙二醇化生长激素释放肽2的合成及其生物学活性的研究
    摘要：The purpose of this study was to investigate an efficient synthetic route to the mono-PEGylated growth hormone releasing peptide-2 (GHRP-2) and its biological activity in vivo. The commercially available key PEGylating reagent, mPEG-NHS ester, was successfully utilized to the synthesis of mono-PEGylated GHRP-2, during which the PEGylation profiles of GHRP-2 were monitored by high-performance liquid chromatography (HPLC). The product was purified by cation exchange chromatography, and its biological activity was conducted in rats. The desired mono-PEGylated GHRP-2 as the major product was readily obtained in anhydrous aprotic solvent, such as dimethyl formamide (DMF) and dimethylsulfoxide (DMSO), when the molar ratio of mPEG-NHS ester to GHRP-2 was fixed to be 0.8:1. The products were characterized by matrix-assisted laser desorption ionization time-of-flight (MALDI-TOF) mass spectrometry. The evaluation of the biological activity for the products showed that the mono-PEGylated GHRP-2 gave a more stable activity than GHRP-2, suggesting that PEGylation led to the increase in the half-life of GHRP-2 in plasma without greatly impairing the biological activity. PEGylation of the GHRP-2 is a good choice for the development of the GHRP-2 applications.
  • 11.

    【2hr】A Study on the Impact of Hydroxypropyl Methylcellulose on the Viscosity of PEG Melt Suspensions Using Surface Plots and Principal Component Analysis

    包量

    机译 用表面图和主成分分析研究羟丙基甲基纤维素对PEG熔体悬浮液粘度的影响
    摘要：An understanding of the rheological behaviour of polymer melt suspensions is crucial in pharmaceutical manufacturing, especially when processed by spray congealing or melt extruding. However, a detailed comparison of the viscosities at each and every temperature and concentration between the various grades of adjuvants in the formulation will be tedious and time-consuming. Therefore, the statistical method, principal component analysis (PCA), was explored in this study. The composite formulations comprising polyethylene glycol (PEG) 3350 and hydroxypropyl methylcellulose (HPMC) of ten different grades (K100 LV, K4M, K15M, K100M, E15 LV, E50 LV, E4M, F50 LV, F4M and Methocel VLV) at various concentrations were prepared and their viscosities at different temperatures determined. Surface plots showed that concentration of HPMC had a greater effect on the viscosity compared to temperature. Particle size and size distribution of HPMC played an important role in the viscosity of melt suspensions. Smaller particles led to a greater viscosity than larger particles. PCA was used to evaluate formulations of different viscosities. The complex viscosity profiles of the various formulations containing HPMC were successfully classified into three clusters of low, moderate and high viscosity. Formulations within each group showed similar viscosities despite differences in grade or concentration of HPMC. Formulations in the low viscosity cluster were found to be sprayable. PCA was able to differentiate the complex viscosity profiles of different formulations containing HPMC in an efficient and time-saving manner and provided an excellent visualisation of the data.
  • 12.

    【2hr】Solid-State Interactions at the Core-Coat Interface: Physicochemical Characterization of Enteric-Coated Omeprazole Pellets Without a Protective Sub-Coat

    包量

    机译 核心-外套界面上的固态相互作用：肠溶衣奥美拉唑小丸无保护底衣的理化特性
    摘要：Conventionally, scanning electron or transmission microscopy, Raman and near infrared (NIR) spectroscopy, terahertz, florescence, and nuclear magnetic resonance imaging have been used to characterize functional coating structure. This study highlights the use of fluorescence microscopy to investigate the physicochemical stability and coating integrity of the commercially available enteric-coated omeprazole pellets containing a basic excipient and prepared by extrusion and spheronization or drug layering on the nonpareil seed, immediately followed by enteric coating (i.e., absence of protective sub-coat). The nature of coating interface and the likely development of an in situ interfacial layer after the application of enteric coating solution was examined using HPLC, NMR, differential scanning calorimetry (DSC), and fluorescent imaging methods. Likewise for the characterization of the solid pellet structure via fluorescence microscopy, a new approach based on fracturing technique (to avoid surface contamination) rather than microtome sectioning was used and validated. Analytical data showed that the pellets containing omeprazole remained chemically stable (>99.5% recovered). Control of the microenvironmental pH by the addition of alkalinizing excipient within a core formulation or as part of drug layering on top of nonpareil seed appears to efficiently neutralize the acidic effect of enteric coating dispersion. Fluorescence images further illustrate the absence of any discernable in situ layer formation at the coat-core interface.
  • 13.

    【2hr】A Reaction of Aspirin with Ferrous Gluconate

    包量

    机译 阿司匹林与葡萄糖酸亚铁的反应
    • 作者：Jian Zhang
    • 刊名：AAPS PharmSciTech
    • 2015年第6期
    摘要：A color reaction of aspirin with ferrous gluconate was studied by UV-Vis spectrophotometry and HPLC-MS. It was found that the UV-Vis spectra of the two drugs were different before and after they were mixed in water at about 0.3 M (diluted by >20 times for analysis), indicating that a complexation reaction took place. The drug-iron complex dissociated when the reacting solution was diluted by 400 times. The by-products of the reaction identified by HPLC-MS were salicylic acid, acetylated gluconic acid, salicylate-gluconic acid conjugate, and an oxidized product of salicylic acid that was complexed with iron with a molecular weight of 212. This reaction may be used as an important consideration to optimize the dosing regime of the two drugs and to help explain some pharmacological reactions between aspirin and biomolecules.
  • 14.

    【2hr】Effect of Cyclodextrins on Morphology and Barrier Characteristics of Isolated Rabbit Corneas

    包量

    机译 环糊精对离体兔角膜细胞形态和屏障特性的影响
    摘要：The objective of the present study is to investigate the confounding effects, if any, of beta-cyclodextrins (βCDs) on corneal permeability coefficients obtained from in vitro transmembrane diffusion studies. Transcorneal permeability studies were carried out with 2-hydroxypropyl-beta-cyclodextrin (HPβCD) and randomly methylated-beta-cyclodextrin (RMβCD) at 5 and 2.5%w/v in isotonic phosphate-buffered solution (IPBS) (pH 7.4). Rabbit corneas received from Pel-Freez Biologicals® were used for these studies. Propranolol hydrochloride (PHCl) (1 mg/mL) was used as the paracellular permeability marker. A series of permeation studies were carried out with IPBS as the control, with CDs on the donor side only, CDs on the receiver side only, and CDs on both the donor and receiver sides. At the end of 1 or 3 h, corneas were collected and fixed using a solution containing 2%v/v glutaraldehyde + 2%w/v paraformaldehyde + IPBS and histological examinations were performed (Excalibur Pathology, Inc). The order of transcorneal permeability of PHCl was found to be CDs on the receiver side > control (no CDs) ≈ CDs on both the receiver and donor sides > CDs on the donor side. Histology studies revealed that the corneal epithelial and endothelial layers remained intact in the control sets. Damage to the cornea was observed in the order of CDs on the receiver side > CDs on the donor side > CDs on both sides > control. The use of CDs in solutions for in vitro permeation experiments with rabbit corneas needs to be carefully considered to avoid confounding effects in the data obtained.
  • 15.

    【2hr】Development of Duloxetine Hydrochloride Loaded Mesoporous Silica Nanoparticles: Characterizations and In Vitro Evaluation

    包量

    机译 盐酸度洛西汀中孔二氧化硅纳米粒子的开发：表征和体外评估。
    摘要：This study investigated the potential use of mesoporous silica nanoparticles (MSNs) as a carrier for duloxetine hydrochloride (DX), which is prone to acid degradation. Sol–gel and solvothermal methods were used to synthesize the MSNs, which, after calcination and drug loading, were then characterized using X-ray diffraction (XRD), Brunauer-Emmett-Teller (BET) technique, thermogravimetric analysis (TGA), Fourier transform infrared (FT-IR) spectroscopy, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and diffuse reflectance ultraviolet-visible (DRS-UV-Vis) spectroscopy. Releases of DX from the MSNs were good in pH 7.4 (90%) phosphate buffer but poor in acidic pH (40%). In a comparative release study between the MSNs in phosphate buffer, TW60-3DX showed sustained release for 140 h, which was higher than the other nanoparticles. The mechanism of DX release from the MSNs was studied using Peppas kinetics model. The “n” value of all three MSNs ranged from 0.45 to 1 with a correlation coefficient (r2) >0.9, which indicated that the release of the drug from the system follows the anomalous transport or non-Fickian diffusion. The results supported the efficacy of mesoporous silica nanoparticles synthesized here as a promising carrier for duloxetine hydrochloride with higher drug loading and greater pH-sensitive release.Electronic supplementary materialThe online version of this article (doi:10.1208/s12249-014-0273-x) contains supplementary material, which is available to authorized users.
  • 16.

    【2hr】Erratum to: Tolerability of High-Volume Subcutaneous Injections of a Viscous Placebo Buffer: A Randomized, Crossover Study in Healthy Subjects

    包量

    机译 勘误表：高剂量皮下注射粘性安慰剂缓冲液的耐受性：健康受试者的随机，交叉研究
    摘要：
  • 17.

    【2hr】Development of Acid-Resistant Alginate/Trimethyl Chitosan Nanoparticles Containing Cationic β-Cyclodextrin Polymers for Insulin Oral Delivery

    包量

    机译 含阳离子β-环糊精聚合物的耐酸藻酸盐/三甲基壳聚糖纳米粒子的胰岛素口服给药研究
    摘要：In this study, the use of trimethylchitosan (TMC), by higher solubility in comparison with chitosan, in alginate/chitosan nanoparticles containing cationic β-cyclodextrin polymers (CPβCDs) has been studied, with the aim of increasing insulin uptake by nanoparticles. Firstly, TMCs were synthesized by iodomethane, and CPβCDs were synthesized within a one-step polycondensation reaction using choline chloride (CC) and epichlorohydrine (EP). Insulin–CβCDPs complex was prepared by mixing 1:1 portion of insulin and CPβCDs solutions. Then, nanoparticles prepared in a three-step procedure based on the iono-tropic pregelation method. Nanoparticles screened using experimental design and Placket Burman methodology to obtain minimum size and polydispercity index (pdI) and the highest entrapment efficiency (EE). CPβCDs and TMC solution concentration and pH and alginate and calcium chloride solution concentrations are found as the significant parameters on size, PdI, and EE. The nanoparticles with proper physicochemical properties were obtained; the size, PdI, and EE% of optimized nanoparticles were reported as 150.82 ± 21 nm, 0.362 ± 0.036, and 93.2% ± 4.1, respectively. The cumulative insulin release in intestinal condition achieved was 50.2% during 6 h. By SEM imaging, separate, spherical, and nonaggregated nanoparticles were found. In the cytotoxicity studies on Caco-2 cell culture, no significant cytotoxicity was observed in 5 h of incubation, but after 24 h of incubation, viability was decreased to 50% in 0.5 mμ of TMC concentration. Permeability studies across Caco-2 cells had been carried out, and permeability achieved in 240 min was 8.41 ± 0.39%, which shows noticeable increase in comparison with chitosan nanoparticles. Thus, according to the results, the optimized nanoparticles can be used as a new insulin oral delivery system.
  • 18.

    【2hr】Dissolution Testing for Bioavailability of Over-the-Counter (OTC) Drugs—a Technical Note

    包量

    机译 非处方药（OTC）生物利用度的溶出度测试-技术说明
    摘要：
  • 19.

    【2hr】Investigating Transdermal Delivery of Vitamin D3

    包量

    机译 研究维生素D3的经皮递送
    摘要：Transdermal delivery of therapeutic amounts of vitamin D3 is proposed to overcome its variable oral bioavailability, especially for people who suffer from fat malabsorption. The main challenge for this delivery route is to overcome the barrier properties of skin, especially for very lipophilic compounds such as vitamin D3. In this study, the effect of different penetration enhancers, such as oleic acid, dodecylamine, ethanol, oleic acid in propylene glycol, isopropyl myristate, octyldodecanol, and oleyl alcohol in propylene glycol were evaluated in vitro for their effectiveness in delivering vitamin D3 through polyamide filter, polydimethylsiloxane membrane, and porcine skin. A diffusion cell was used to study the transdermal permeability of vitamin D3. Ointment formulations of vitamin D3 were prepared containing the most widely used penetration enhancers, oleic acid, and dodecylamine. The ointment containing oleic acid as chemical penetration enhancer did not improve delivery compared to control. On the other hand, the formulation containing dodecylamine as a penetration enhancer did improve the transdermal delivery of vitamin D3. However, statistical significance and an amount high enough for nutritional supplementation purposes were reached only when the skin was pretreated with 50% ethanol. In these conditions, the ointment delivered an amount of 760-ng vitamin D3 per cm2 of skin. The research shows promise that transdermal delivery could be an effective administration route for vitamin D3 when ethanol and dodecylamine are used as penetration enhancers.
  • 20.

    【2hr】The Anti-Melanoma Efficiency of the Intratumoral Injection of Cucurbitacin-Loaded Sustained Release Carriers: In Situ-Forming Implants

    包量

    机译 葫芦素缓释载体瘤内注射的抗黑素瘤效率：原位形成植入物。
    摘要：Our previous studies revealed that the PLGA-based particulate systems loaded with cucurbitacin showed limited anti-melanoma efficiency in xenograft animal models after intratumoral injection, which was due to the undesirable initial burst release and the leakage of the particulate carriers from the injection site through the pinhole. In this paper, two categories of in situ-forming implants (ISFIs) for intratumoral injection, PLGA ISFIs and SAIB ISFIs, were systemically evaluated for their potentials for on solid tumor treatment via intratumoral injection. The in vitro drug release profiles of these two ISFIs were different due to the different sol–gel transition properties. The pharmacodynamics results revealed that SAIB ISFIs displayed obvious therapeutic efficiencies to melanoma, and multi-points injection of SASIB ISFIs displayed better efficiency than single-point injection. The different sol–gel transition properties and mechanism for PLGA ISFIs and SAIB ISFIs affected both the drug release and strongly impacted the pharmacokinetic parameters and pharmacodynamic effectiveness. Also, the adhesive property of SAIB to the local tissue could extend the retention and inhibit the leakage of the SAIB ISFIs, thus enhanced the anticancer effectiveness. Comparison of the various intratumoral injection systems, appropriate drug release profiles (lower initial burst and steady release) and good retention (minimum leakage from the injection site) would benefit to the antitumor effects of the intratumoral depots.Electronic supplementary materialThe online version of this article (doi:10.1208/s12249-015-0292-2) contains supplementary material, which is available to authorized users.
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