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European Journal of Pharmaceutics and Biopharmaceutics

Shiqi Lin, Bingzhen Cai, Guilan Quan, Tingting Peng, Gangtao Yao, Chune Zhu, Qiaoli Wu, Hao Ran, Xin Pan, Chuanbin Wu
Thymopentin (TP5) is commonly used in the treatment for autoimmune diseases, with a short plasma half-life (30 s) and a long treatment period (7 days to 6 months). It is usually administrated by syringe injection, resulting in compromised patient compliance. Dissolving microneedle array (DMNA) offers a superior approach for transdermal delivery of biological macromolecules, as it allows painless penetration through the stratum corneum and generates minimal biohazardous waste after dissolving in the skin. Despite recent advances in DMNA as a novel approach for transdermal drug delivery, problem of insufficient mechanical strength remains to be solved...
October 14, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Paola Mura, Natascia Mennini, Cristina Nativi, Barbara Richichi
Previous studies proved the effectiveness of an intravenous PEGylated liposomal formulation of opiorphin (1 mg/mL) in protecting the drug from enzymatic degradation, and improving intensity and duration of its painkilling effect. Therefore, considering the advantages of nasal administration, the aim of this work was the development of a liposomal mucoadhesive thermo-sensitive in situ gel for the extended nasal delivery of opiorphin. With this purpose, the potential of a series of combinations of different polymers (i...
October 12, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Qian Xie, Wenji Deng, Xue Yuan, Huan Wang, Zhiguo Ma, Baojian Wu, Xingwang Zhang
Liposomes have shown to be an excellent drug delivery system, but the short in vivo fate discourages their popularity. This work aimed to develop selenium-functionalized liposomes (SeLPs) for doxorubicin (Dox) delivery to prolong the systemic circulation of liposomes by in situ selenium coating and enhance the anticancer effect via the synergy between Dox and selenium. Dox-loaded SeLPs (Dox-SeLPs) were prepared by film hydration/active loading/in situ reduction technique and characterized by particle size, entrapment efficiency and morphology...
October 12, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Anita K Bakrania, Bhavesh C Variya, Lalji V Rathod, Snehal S Patel
Triple negative breast cancer revolution has identified a plethora of therapeutic targets making it apparent that a single target for its treatment could be rare hence creating an urge to develop robust technologies for combination drug therapy. Paclitaxel, hailed as the most significant advancement in chemotherapy faces several underpinnings due to its low solubility and permeability. Advancing research has demonstrated the role of interferons in cancer. DEAE-Dextran, an emerging molecule with evidence of interferon induction was utilized in the present study to develop a nanoformulation in conjugation with paclitaxel to target multiple therapeutic pathways, with diminution of paclitaxel adverse effects and develop a specific targeted nano system...
October 11, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Roxana E Ghitescu, Ana Maria Popa, Angela Schipanski, Cordula Hirsch, Gökce Yazgan, Valentin I Popa, René M Rossi, Katharina Maniura-Weber, Giuseppino Fortunato
Reactive oxygen species (ROS) are common products of normal aerobic cellular metabolism, but high levels of ROS lead to oxidative stress and cellular damage. Therefore, effective antioxidant therapies are needed to prevent ROS overproduction. This study reports the development of poly(l-lactide-co-glycolide) (PLGA) bicomponent fibers loaded with selected amounts of the natural polyphenolic antioxidant catechin. Thereby a novel route based on emulsion electrospinning is investigated to obtain tailored and sustained release rates for chatechin...
October 11, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Parind M Desai, Vibha Puri, David Brancazio, Bhakti S Halkude, Jeremy E Hartman, Aniket V Wahane, Alexander R Martinez, Keith D Jensen, Eranda Harinath, Richard D Braatz, Jung-Hoon Chun, Bernhardt L Trout
We developed and evaluated a solvent-free injection molding (IM) coating technology that could be suitable for continuous manufacturing via incorporation with IM tableting. Coating formulations (coating polymers and plasticizers) were prepared using hot-melt extrusion and screened via stress-strain analysis employing a universal testing machine. Selected coating formulations were studied for their melt flow characteristics. Tablets were coated using a vertical injection molding unit. Process parameters like softening temperature, injection pressure, and cooling temperature played a very important role in IM coating processing...
October 9, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Lili Duse, Shashank Reddy Pinnapireddy, Boris Strehlow, Jarmila Jedelská, Udo Bakowsky
Oncological use of photodynamic therapy is an evolving field in cancer therapeutics. Photosensitisers are prone to accumulation inside healthy tissues causing undesirable effects. To avoid this, we have developed tetraether lipid liposomal formulations containing curcumin which is a naturally occurring anti-cancer substance and deemed to be safe towards healthy cells. Upon excitation with light at a specific wavelength, curcumin produces reactive oxygen species (ROS) in presence of oxygen, thereby exhibiting a cytotoxic effect towards the surrounding tissues, giving a total control on the onset of therapy...
October 7, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Xianpeng Shi, Yan Yan, Pengchong Wang, Ying Sun, Di Zhang, Yamin Zou, Sasa Hu, Lu Zhang, Jianfeng Xing, Yalin Dong
Hydrocortisone sodium succinate (HSS) is an anti-inflammatory drug, but its application on ulcerative colitis (UC) treatment is limited by its associated side-effects. To solve this problem, a kind of pH-sensitive P(LE-IA-MEG) hydrogel microspheres (HMSs) were prepared as the drug carrier of hydrocortisone sodium succinate (HSS) for the treatment of UC. The P(LE-IA-MEG) HMSs were spherical in shape with good dispersion and the mean particle size was 34.87 ± 0.90 µm. HSS was successfully loaded into the P(LE-IA-MEG) HMSs...
October 7, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Maria Summa, Debora Russo, Ilaria Penna, Natasha Margaroli, Ilker S Bayer, Tiziano Bandiera, Athanassia Athanassiou, Rosalia Bertorelli
In the last few years, there has been an increasing tendency to use natural polymers for the fabrication of dressings for wound and burn management. Among them, alginate, a polysaccharide extracted primarily from marine algae, exhibits attractive properties being non-toxic, hydrophilic and biodegradable. The aim of this study was to characterize the in vitro biocompatibility and the efficacy of a composite polymeric material based on sodium alginate (NaAlg) and povidone iodine (PVPI) complex in a mouse model of wound healing...
October 7, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Shunsuke Kimura, Akiko Kiriyama, Kaeko Araki, Mai Yoshizumi, Masakazu Enomura, Daisuke Inoue, Tomoyuki Furubayashi, Reiko Yutani, Reiko Teraoka, Akiko Tanaka, Kosuke Kusamori, Hidemasa Katsumi, Akira Yamamoto, Katsumi Iga, Toshiyasu Sakane
Amorphization has been widely recognized as a useful solubilization technique for poorly water-soluble drugs, such as curcumin. We have recently reported the novel finding that the membrane transport of curcumin was markedly enhanced when amorphous solid particles of curcumin came into direct contact with the lipid membrane surface, but this was not true for crystalline solid particles. The increase in the permeation of curcumin was found to be independent of the improvements in aqueous solubility brought about by amorphization...
October 5, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Luisa Stella Dolci, Silvia Panzavolta, Beatrice Albertini, Barbara Campisi, Massimo Gandolfi, Adriana Bigi, Nadia Passerini
The aim of this work was to develop an innovative drug delivery system potentially useful for the local delivery of Bisphosphonates to bone tissue. We propose the use of Solid Lipid Microparticles (MPs), up to now mainly used for oral and topical drug delivery, as carrier for bisphosphonates due to the favourable biocompatibility and lower toxicity of the lipids compared with many polymers. The delivery platform consisted of a biomimetic α-tricalcium phosphate-gelatin cement (CPC) enriched with alendronate loaded MPs (MPs-AL) produced by the spray congealing technology...
October 3, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Maria Doreth, Korbinian Löbmann, Petra Priemel, Holger Grohganz, Robert Taylor, René Holm, Heidi Lopez de Diego, Thomas Rades
In situ amorphization is an approach that enables a phase transition of a crystalline drug to its amorphous form immediately prior to administration. In this study, three different polyvinylpyrrolidones (PVP K12, K17 and K25) were selected to investigate the influence of the molecular weight of the polymer on the degree of amorphization of the model drug indomethacin (IND) upon microwaving. Powder mixtures of crystalline IND and the respective PVP were compacted at 1:2 (w/w) IND:PVP ratios, stored at 54% RH and subsequently microwaved with a total energy input of 90 or 180 kJ...
October 3, 2017: European Journal of Pharmaceutics and Biopharmaceutics
David Lucio, María Cristina Martínez-Ohárriz, Gonzalo Jaras, Paula Aranaz, Carlos J González-Navarro, Aurel Radulescu, Juan M Irache
The aim of this work was to evaluate the capability of zein nanoparticles as oral carriers for glibenclamide (GB). Nanoparticles were prepared by a desolvation procedure in the presence of lysine as stabilizer. A central composite design was used to optimize this preparative process. Under the selected conditions, nanoparticles displayed a size of about 190 nm, a surface charge of -37 mV and a payload of 45 µg GB/mg. Small-angle neutron scattering and X-ray diffraction techniques suggested an internal fractal-like structure, based on the repetition of spherical blocks of zein units (about 20 nm) grouped to form the nanoparticles...
October 3, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Eva Marxen, Mette Dalskov Mosgaard, Anne Marie Lynge Pedersen, Jette Jacobsen
The mucus layer is believed to play a part in drug permeation across the oral mucosa. Human freeze-dried saliva (HFDS) and porcine gastric mucin (PGM) was evaluated as model for mucus layer per se or in conjunction with in vitro and ex vivo buccal permeability models. Four small molecules (nicotine, mannitol, propranolol, caffeine) showed decreased permeability across mucin dispersions, compared to controls, and a greater effect was seen with HFDS than with PGM. Permeability of propranolol and caffeine across filter-grown TR146 cells was decreased by the presence of mucin, whereas no effect was found on nicotine and mannitol...
September 30, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Masateru Miyake, Satoshi Kondo, Toshihisa Koga, Noriaki Yoda, Satoru Nakazato, Chie Emoto, Tadashi Mukai, Hajime Toguchi
The purpose of this study was to evaluate the intestinal metabolism and absorption in a mini-Ussing chamber equipped with animal intestinal tissues, based on the transport index (TI). TI value was defined as the sum of drug amounts transported to the basal-side component (X(corr)) and drug amounts accumulated in the tissue (T(corr)), which are normalized by AUC of a drug in the apical compartment, as an index for drug absorption. Midazolam was used as a test compound for the evaluation of intestinal metabolism and absorption...
September 30, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Armando Chierchia, Nino Chirico, Lucia Boeri, Ilaria Raimondi, Giovanni A Riva, Manuela Teresa Raimondi, Marta Tunesi, Carmen Giordano, Gianluigi Forloni, Diego Albani
Neurodegenerative diseases, as Parkinson's disease (PD), involve irreversible neural cell damage and impairment. In PD, there is a selective degeneration of the dopaminergic neurons leading to motor symptoms. A common finding in PD neurodegeneration is the increase of reactive oxygen species (ROS), leading to oxidative stress. To date there are only interventions to relieve PD symptoms, however progress has been made in the development of therapies that target the immune system or use its components as therapeutic agents; among these, mesenchymal stem cells (MSCs), which are able to express neuroprotective factors as cytokines, chemokines and angiogenic molecules, collectively named secretome, that accumulate in MSC culture medium...
September 28, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Moritz C Rehbein, Sascha Husmann, Christian Lechner, Conrad Kunick, Stephan Scholl
In early stages of drug development only sparse amounts of the key substances are available, which is problematic for the determination of important process data like reaction kinetics. Therefore, it is important to perform experiments as economically as possible, especially in regards to limiting compounds. Here we demonstrate the use of a temperature step experiment enabling the determination of complete reaction kinetics in a single non-isothermal experiment. In contrast to the traditionally used HPLC, the method takes advantage of the high measuring rate and the low amount of labor involved in using in-situ ATR-FTIR to determine time-dependent concentration-equivalent data...
September 26, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Avital Beig, Noa Fine-Shamir, Daniel Porat, David Lindley, Jonathan M Miller, Arik Dahan
Vitamin E TPGS (TPGS) has both surfactant and P-glycoprotein (P-gp) inhibitory effects. While surfactants were previously found to cause solubility-permeability tradeoff, TPGS P-gp inhibitory effects may change this unfavorable interplay. The purpose of this research was to investigate the solubility-permeability interplay when using TPGS vs. amorphous solid dispersions (ASD) as oral drug delivery systems for the anticancer, P-gp substrate, lipophilic drug etoposide. The concentration-dependent effects of TPGS (0-100 mg/mL) vs...
September 25, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Fatemeh Saeidipour, Zahra Mansourpour, Elaheh Mortazavian, Niyousha Rafiee-Tehrani, Morteza Rafiee-Tehrani
A comprehensive model with all effective phenomena in drug release such as diffusion, swelling and erosion was considered. In this work, a mathematical model was developed to describe drug release from controlled release HPMC matrices as a favorable system in pharmaceutical industries. As a novel study, the impact of the MCC presence as a filler in tablet preparation process was considered in the mathematical model. In addition, we found that the volume expansion of these polymeric matrices did not follow the ideal mixing rule and we derived an equation for estimating the volume of hydrated matrix...
September 22, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Bär David, Debus Heiko, Grune Christian, Tosch Stephan, Fischer Wolfgang, Mäder Karsten, Imming Peter
Naproxen is a typical and well-known analgesic classified as non-steroidal anti-inflammatory drug (NSAID) and is commercialized as tablets or liquid-filled capsules. Naproxen is typically used as a sodium salt because of its better processability compared to Naproxen free acid. This entails hygroscopicity and gives rise to the existence of four different hydrates, which show polymorphic and pseudopolymorphic properties. Solid dosage forms containing Naproxen Sodium often have to be processed in an applicable dosage form by granulation and tablet compression...
September 19, 2017: European Journal of Pharmaceutics and Biopharmaceutics
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