Design and characterisation of electrospun shellac-polyvinylpyrrolidone blended micro/nanofibres loaded with monolaurin for application in wound healing
Publication date: Available online 22 March 2019Source: International Journal of PharmaceuticsAuthor(s): Nawinda Chinatangkul, Sukannika Tubtimsri, Danuch Panchapornpon, Prasert Akkaramongkolporn, Chutima Limmatvapirat, Sontaya LimmatvapiratAbstractDue to their ultrafine network structures, electrospun nanofibres have been potentially used for wound application. In order to develop a desired wound dressing material, shellac (SHL) was blended with polyvinyl pyrrolidone (PVP). Monolaurin (ML), which is a natural antimicrobial lipid, was incorporated into the SHL-PVP blended fibres to prevent delayed wound healing resulting f...
Source: International Journal of Pharmaceutics - March 23, 2019 Category: Drugs & Pharmacology Source Type: research

Developing methodology to evaluate the oral sensory features of pharmaceutical tablet coatings
This study demonstrates that slippery coatings improve acceptability of tablets. The study also demonstrates the value of VAS to measure the sensory attributes of coated tablets.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - March 22, 2019 Category: Drugs & Pharmacology Source Type: research

Conjugation of a peptide autoantigen to gold nanoparticles for intradermally administered antigen specific immunotherapy
In this study we have covalently attached an autoantigen, currently under clinical evaluation for the treatment of type 1 diabetes (PIC19-A3 peptide), to AuNPs to create nanoscale (
Source: International Journal of Pharmaceutics - March 22, 2019 Category: Drugs & Pharmacology Source Type: research

Copper sulfide: an emerging adaptable nanoplatform in cancer theranostics
This article discusses the pros and cons of using CuS NPs in diagnostics, therapeutics, and theranostics. The first section introduces CuS NPs and discusses the features that render them more advantageous than other established nanoplatforms in cancer management. Subsequent sections include specific in vitro and in vivo results of different studies showing the potential of CuS NPs as nanoplatforms. Methods used for visualization (photoacoustic imaging and magnetic resonance imaging) of CuS NPs and treatment (phototherapy and combinatorial therapy) have also been discussed. Furthermore, the challenges and opportunities asso...
Source: International Journal of Pharmaceutics - March 22, 2019 Category: Drugs & Pharmacology Source Type: research

Rice starch thin films as a potential buccal delivery system: Effect of plasticiser and drug loading on drug release profile
This study focuses on investigating the impact of plasticiser and drug loading on drug release pattern of rice starch films which has not been explored to date. The obtained rice films were characterised for their physicochemical properties including swelling and dissolution study. The highest drug dissolution rate was achieved in the rice films with a low drug loading due to drug amorphicity in nature. When drug loading increases, the swelling behaviour of rice films plays a dominant role in releasing drug in the crystalline form. The role of plasticiser was indicated by the plasticiser-starch interaction where a strong i...
Source: International Journal of Pharmaceutics - March 22, 2019 Category: Drugs & Pharmacology Source Type: research

Investigating the effect and mechanism of particle size distribution variability on mixing using avalanche testing and multivariate modelling
This study yielded three conclusions. Firstly, PSD variability in pharmaceutical grade excipients can cause unacceptable prolongation in mixing time. Secondly, the impact of PSD variability on continuous mixing and other batch mixing of various scales, requires investigation. Lastly, the current findings can contribute to the development of robust mixing operations in the form of offline pre-emptive measures and inline process control strategies.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - March 22, 2019 Category: Drugs & Pharmacology Source Type: research

Artesunate-heparin conjugate based nanocapsules with improved pharmacokinetics to combat malaria
In conclusion, such multifunctional ART-HEP-NCPs with higher ART loading and extended half-life could be a promising platform for targeted antimalarial drug delivery.Graphical abstractChemical structure of ART-conjugated heparin, its self-assembly and delivery to iRBCs. (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - March 20, 2019 Category: Drugs & Pharmacology Source Type: research

Comparative assessment of efficacy and safety potential of multifarious lipid based Tacrolimus loaded nanoformulations
Publication date: Available online 19 March 2019Source: International Journal of PharmaceuticsAuthor(s): Sanyog Jain, Ramu Addan, Varun Kushwah, Harshad Harde, Rahul R. MahajanAbstractThe present work reports the development, optimization and characterization of novel lipid based nanoformulations viz., Liquid crystalline nanoparticles (LCNP), solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) and liposomes loaded with Tacrolimus (Tac) for topical delivery. Different nanoformulations were developed after screening lipids and suitable surfactants depending upon emulsification ability. The various nanofor...
Source: International Journal of Pharmaceutics - March 20, 2019 Category: Drugs & Pharmacology Source Type: research

Kinetic stability of amorphous solid dispersions with high content of the drug: a Fast Scanning Calorimetry investigation
Publication date: Available online 19 March 2019Source: International Journal of PharmaceuticsAuthor(s): S.E. Lapuk, L.S. Zubaidullina, M.A. Ziganshin, T.A. Mukhametzyanov, C. Schick, A.V. GerasimovAbstractFormation of amorphous solid dispersions is an effective way to enhance the bioavailability of drugs. One of the main disadvantages of such systems is their low storage stability. Estimation and prognosis of storage stability of the amorphous solid dispersions are possible through modeling of the kinetics of crystallization by the Arrhenius equation and the resulting parameters, i.e., activation energy and pre-exponentia...
Source: International Journal of Pharmaceutics - March 20, 2019 Category: Drugs & Pharmacology Source Type: research

Evaluation of size and dose effects of rChe a 3 allergen loaded PLGA nanoparticles on modulation of Th2 immune responses by sublingual immunotherapy in mouse model of rhinitis allergic
Publication date: Available online 19 March 2019Source: International Journal of PharmaceuticsAuthor(s): Jafar Hajavi, Maryam hashemi, Mojtaba SankianGraphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - March 20, 2019 Category: Drugs & Pharmacology Source Type: research

Evaluation of various tissue-clearing techniques for the three-dimensional visualization of liposome distribution in mouse lungs at the alveolar scale
ConclusionsThese results suggest that the ClearT2 tissue-clearing technique was appropriate for the three-dimensional visualization of intrapulmonary liposomes at the alveolar scale. This study provides important information for selecting and optimizing suitable optical tissue-clearing techniques in lungs for evaluating the distribution of pulmonary drug delivery systems.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - March 20, 2019 Category: Drugs & Pharmacology Source Type: research

Tunable drug release from blend poly(vinyl pyrrolidone)-ethyl cellulose nanofibers
Publication date: Available online 18 March 2019Source: International Journal of PharmaceuticsAuthor(s): V. Umayangana Godakanda, Heyu Li, Laura Alquezar, Lixiang Zhao, Li-Min Zhu, Rohini de Silva, K.M. Nalin de Silva, Gareth R. WilliamsAbstractThe management of pain and inflammation arising from wounds is essential in obtaining effective healing rates. The application of a wound dressing loaded with an anti-inflammatory drug would enable both issues to be ameliorated, and the aim of this work was to fabricate such a dressing by electrospinning. Fibers comprising ethyl cellulose (EC) and poly(vinyl pyrrolidone) (PVP) loade...
Source: International Journal of Pharmaceutics - March 19, 2019 Category: Drugs & Pharmacology Source Type: research

Curcumin nanoparticles containing poloxamer or soluplus tailored by high pressure homogenization using antisolvent crystallization
In conclusion, samples crystalized and proceed with HPH technique showed smaller particle size, better re-dispersibility, higher solubility and dissolution rate in water compared with a sample prepared using a simple antisolvent crystallization process.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - March 19, 2019 Category: Drugs & Pharmacology Source Type: research

A Surfactant-like Chemotherapeutic agent as a Nanocarrier for Delivering Photosensitizers against Cancer: A Facile Drug-Delivering-Drug Strategy
Publication date: Available online 18 March 2019Source: International Journal of PharmaceuticsAuthor(s): Zhaomeng Wang, Mengchi Sun, Tian Liu, Xiao Tan, Haotian Zhang, Xiangyu Zhang, Zhonggui He, Jin SunAbstractPhotosensitizer-based photodynamic therapy (PDT) has attracted great attention in cancer treatment. However, achieving efficient delivery of photosensitizers is still a great challenge for their clinical applications. The photosensitizer-encapsulating delivery nanosystem usually suffers from poor stability, complex preparation process and low drug loading. Herein, we utilize a surfactant-like chemotherapeutic agent,...
Source: International Journal of Pharmaceutics - March 19, 2019 Category: Drugs & Pharmacology Source Type: research

Development and in vitro characterization of an oral self-emulsifying delivery system (SEDDS) for rutin fatty ester with high mucus permeating properties
Publication date: Available online 18 March 2019Source: International Journal of PharmaceuticsAuthor(s): Maria I. Cardona, Nguyet-Minh Nguyen Le, Sergey Zaichik, Diana M. Aragón, Andreas Bernkop- SchnürchAbstractThe aim of this study was to develop and evaluate a self-emulsifying delivery system (SEDDS) for oral rutin fatty ester administration and to improve its mucus permeating properties by the incorporation of the silicon polymer poly [dimethylsiloxane-co-(3-(2-(2-hydroxyethoxy)ethoxy)propyl]methylsiloxane] (PDMSHEPMS) in the formulation. In order to increase the lipophilicity of the flavonoid and to dissol...
Source: International Journal of Pharmaceutics - March 19, 2019 Category: Drugs & Pharmacology Source Type: research

Rapid sample-saving biophysical characterisation and long-term storage stability of liquid interferon alpha2a formulations: Is there a correlation?
Publication date: 1 May 2019Source: International Journal of Pharmaceutics, Volume 562Author(s): Hristo Svilenov, Gerhard WinterAbstractThe knowledge and tools to characterise proteins have comprehensively developed in the last two decades. Some of these tools are used in formulation development to select formulation conditions suitable for long-term storage. However, there is an ongoing debate whether the predictions obtained with these tools are in good agreement with the outcome from real-time long-term stability studies. In this work, we investigate whether some of the state-of-the-art microscale, microvolume and non d...
Source: International Journal of Pharmaceutics - March 19, 2019 Category: Drugs & Pharmacology Source Type: research

1H NMR quantification of spray dried and spray freeze-dried saccharide carriers in dry powder inhaler formulations
Publication date: Available online 16 March 2019Source: International Journal of PharmaceuticsAuthor(s): Mai Babenko, Jean-Marie R. Peron, Waseem Kaialy, Gianpiero Calabrese, Raid G. Alany, Amr ElShaerAbstractQuantitative analysis using proton NMR (1H qNMR) has been employed in various areas such as pharmaceutical analysis (e.g., dissolution study), vaccines, natural products analysis, metabolites, and macrolide antibiotics in agriculture industry. However, it is not routinely used in the quantification of saccharides in dry powder inhaler (DPI) formulations. The aim of this study was to develop a 1H NMR method for the qua...
Source: International Journal of Pharmaceutics - March 17, 2019 Category: Drugs & Pharmacology Source Type: research

Preparation, in vitro and in vivo Evaluation of Isoliquiritigenin-loaded TPGS modified proliposomes
Publication date: Available online 16 March 2019Source: International Journal of PharmaceuticsAuthor(s): Jian Liu, Qilong Wang, Michael Adu-Frimpong, Qiuyu Wei, Yujiao Xie, Kangyi Zhang, Chunmei Wei, Wen Weng, Hao Ji, Elmurat Toreniyazov, Ximing Xu, Jiangnan YuAbstractIsoliquiritigenin (ISL) has a great variety of pharmacological effects especially liver cancer therapy, but its poor solubility, bioavailability and liver targeting have limited its clinical use. In order to solve the aforementioned shortcomings, the TPGS-modified proliposomes loaded with ISL (ISL-TPGS-PLP) was prepared in this study. ISL-TPGS-PLP was fabrica...
Source: International Journal of Pharmaceutics - March 17, 2019 Category: Drugs & Pharmacology Source Type: research

Flexible two-layer dissolving and safing Microneedle transdermal of Neurotoxin: A biocomfortable attempt to treat Rheumatoid Arthritis
This study is directed towards the gentle transdermal delivery of Neurotoxin (NT) and study of the treatment of Rheumatoid Arthritis (RA) in rats by NT loaded dissolving Microneedles (DMNs-NT). The DMNs-NT fabrication involved a two-step centrifugation method. The quadrangular pyramid shape needles had great mechanical strength. The upper part of the needle contained 15.4±0.5 μg of drug per patch. Blank DMNs showed favorable biocompatibility and low toxicity on the chondrocyte cells. Both NT and DMNs-NT displayed anti-inflammatory capabilities ex-vitro. The results of ex-vitro evaluation of DMNs the skin penetrat...
Source: International Journal of Pharmaceutics - March 17, 2019 Category: Drugs & Pharmacology Source Type: research

Phytoestrogen coumestrol: antioxidant capacity and its loading in albumin nanoparticles
Publication date: Available online 16 March 2019Source: International Journal of PharmaceuticsAuthor(s): Guillermo Montero, Francisco Arriagada, Germán Günther, Soledad Bollo, Francisco Mura, Eduardo Berríos, Javier MoralesAbstractCoumestrol is a polyphenol with promising therapeutic applications as phytoestrogen, antioxidant and potential cancer chemoprevention agent. The presence of two hydroxyl groups on its chemical structure, with orientation analogous to estradiol, is responsible of both, its antioxidant capacity and its estrogenic activity. However, several studies show that the interaction of pol...
Source: International Journal of Pharmaceutics - March 16, 2019 Category: Drugs & Pharmacology Source Type: research

Acrylated Eudragit® E PO as a novel polymeric excipient with enhanced mucoadhesive properties for application in nasal drug delivery
Publication date: Available online 14 March 2019Source: International Journal of PharmaceuticsAuthor(s): Natalia N. Porfiryeva, Shamil F. Nasibullin, Svetlana G. Abdullina, Irina K. Tukhbatullina, Rouslan I. Moustafine, Vitaliy V. KhutoryanskiyAbstractEudragit® E PO (EPO) is a terpolymer based on N,N-dimethylaminoethyl methacrylate with methylmethacrylate and butylmethacrylate, produced by Evonik Industries AG as a pharmaceutical excipient. In this work, EPO was chemically modified through reaction with acryloyl chloride. The successful modification of EPO was confirmed by FTIR, NMR-spectroscopy, elemental and thermal ...
Source: International Journal of Pharmaceutics - March 15, 2019 Category: Drugs & Pharmacology Source Type: research

Optimization of peptide-based cancer vaccine compositions, by sequential screening, using versatile liposomal platform
Publication date: Available online 15 March 2019Source: International Journal of PharmaceuticsAuthor(s): Célia Jacoberger-Foissac, Hanadi Saliba, Cendrine Seguin, Anaïs Brion, Zahra Kakhi, Benoît Frisch, Sylvie Fournel, Béatrice HeurtaultAbstractTherapeutic cancer vaccines need thoughtful design to efficiently deliver appropriate antigens and adjuvants to the immune system. In the current study, we took advantage of the versatility of a liposomal platform to conceive and customize vaccines containing three elements needed for the induction of efficient antitumor immunity: i) a CD4 epitope peptide a...
Source: International Journal of Pharmaceutics - March 15, 2019 Category: Drugs & Pharmacology Source Type: research

Enhanced vitamin C skin permeation from supramolecular hydrogels, illustrated using in situ ToF-SIMS 3D chemical profiling
Publication date: Available online 15 March 2019Source: International Journal of PharmaceuticsAuthor(s): Nichola J. Starr, Khuriah Abdul Hamid, Judata Wibawa, Ian Marlow, Mike Bell, Luïsa Pérez-García, David A. Barrett, David J. ScurrAbstractVitamin C (ascorbic acid) is a naturally occurring, powerful anti-oxidant with the potential to deliver numerous benefits to the skin when applied topically. However, topical use of this compound is currently restricted by an instability in traditional formulations and the delivery and eventual fate of precursor compounds has been largely unexplored. Time of flight s...
Source: International Journal of Pharmaceutics - March 15, 2019 Category: Drugs & Pharmacology Source Type: research

A novel FK506 loaded nanomicelles consisting of amino-terminated poly(ethylene glycol)-block-poly(D,L)-lactic acid and hydroxypropyl methylcellulose for ocular drug delivery
In conclusion, FK506 / NH2-PEG-b-PLA / HPMC NMs formulations as a promising ocular drug delivery system would be able to improve the bioavailability and efficacy of FK506 in anti-allograft rejection.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - March 14, 2019 Category: Drugs & Pharmacology Source Type: research

Fabrication and Evaluation of Dental Fillers Using Customized Molds via 3D Printing Technology
The objective of this study was to fabricate and evaluate novel dental fillers using state-of-the-art 3D printing technology. Tinidazole (TNZ), a commonly used antibacterial drug in the dental clinic, was chosen as the model compound. Models of molars with carious cavities were obtained via 3D scanning. TNZ dental fillers were indirectly produced by thermal pressing using customized 3D printed molds. In addition, bio-relevant in vitro dissolution and mechanical testing methods were developed using customized 3D printed release and compression molds, respectively. It was observed that the formability, mechanical properties,...
Source: International Journal of Pharmaceutics - March 14, 2019 Category: Drugs & Pharmacology Source Type: research

Self-Assembled Hexagonal Liquid Crystalline Gels as Novel Ocular Formulation with Enhanced Topical Delivery of Pilocarpine Nitrate
Publication date: Available online 14 March 2019Source: International Journal of PharmaceuticsAuthor(s): Xingqi Wang, Yong Zhang, Jie Huang, Mengqiu Xia, Liu Liu, Chunling Tian, Rongfeng Hu, Shuangying Gui, Xiaoqin ChuAbstractThe aim of this paper was to develop hexagonal liquid crystalline (HII) gels that can be used as a novel ocular delivery system for pilocarpine nitrate (PN). HII gels were prepared by a vortex method using phytantriol/triglyceride/water (71.15: 3.85: 26, w/w) ternary system. The gels were characterized by crossed polarized light microscopy, small-angle X-ray scattering, differential scanning calorimet...
Source: International Journal of Pharmaceutics - March 14, 2019 Category: Drugs & Pharmacology Source Type: research

Rapid sample-saving biophysical characterization and long-term storage stability of liquid interferon alpha2a formulations: Is there a correlation?
Publication date: Available online 14 March 2019Source: International Journal of PharmaceuticsAuthor(s): Hristo Svilenov, Gerhard WinterAbstractThe knowledge and tools to characterize proteins have comprehensively developed in the last two decades. Some of these tools are used in formulation development to select formulation conditions suitable for long-term storage. However, there is an ongoing debate whether the predictions obtained with these tools are in a good agreement with the outcome from real-time long-term stability studies. In this work, we investigate whether some of the state-of-the-art microscale, microvolume...
Source: International Journal of Pharmaceutics - March 14, 2019 Category: Drugs & Pharmacology Source Type: research

Cp1-11 peptide/insulin complex loaded pH-responsive nanoparticles with enhanced oral bioactivity
Publication date: Available online 12 March 2019Source: International Journal of PharmaceuticsAuthor(s): Xingyu Chen, Yushuang Ren, Ying Feng, Xinyuan Xu, Hong Tan, Jianshu LiAbstractTo improve the oral efficiency of insulin, a novel oral insulin delivery system was developed, to protect the insulin from destruction, and to deliver monomeric insulin with higher bioactivity. The oral insulin delivery system was developed by using chitosan/alginate nanoparticles as carriers for the oral delivery of Cp1-11 peptide/insulin complex (Cp1-11 peptide/Insulin Loaded Nanoparticle, CILN). There is a supramolecular interaction between...
Source: International Journal of Pharmaceutics - March 13, 2019 Category: Drugs & Pharmacology Source Type: research

Application of the QbD-based approach in the early development of liposomes for nasal administration
Publication date: Available online 13 March 2019Source: International Journal of PharmaceuticsAuthor(s): Edina Pallagi, Orsolya Jójárt-Laczkovich, Zsófia Németh, Piroska Szabó-Révész, Ildikó CsókaGraphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - March 13, 2019 Category: Drugs & Pharmacology Source Type: research

Development of a dosing device for individualized dosing of orodispersible warfarin films
This study covers the development of a dosing device that enables flexible dosing of films within the pharmacopoeial requirements. The prototype was produced with the 3D-printing technique fused filament fabrication. The developed and produced prototype of the device was tested for the uniformity of doses according to Ph.Eur. 2.9.27 and 2.9.40. A ribbon as model film and an oral film with HPMC as polymer matrix met the specifications for both tests for three different lengths dispensed with the prototype of the dosing device (HPMC film: AV = 11.30 (1cm), 12.04 (2cm) and 10.19 (3cm)). A second oral film with a pol...
Source: International Journal of Pharmaceutics - March 13, 2019 Category: Drugs & Pharmacology Source Type: research

Carbosilane dendrimers with phosphonium terminal groups are low toxic non-viral transfection vectors for siRNA cell delivery
Publication date: Available online 13 March 2019Source: International Journal of PharmaceuticsAuthor(s): Regina Herma, Dominika Wrobel, Michaela Liegertová, Monika Müllerová, Tomáš Strašák, Marek Maly, Alena Semerádtová, Marcel Štofik, Dietmar Appelhans, Jan MalyAbstractNon-viral gene delivery vectors studied in the gene therapy applications are often designed with the cationic nitrogen containing groups necessary for binding and cell release of nucleic acids. Disadvantage is a relatively high toxicity which restricts the in vivo use of such nanoparticles....
Source: International Journal of Pharmaceutics - March 13, 2019 Category: Drugs & Pharmacology Source Type: research

Polymer-lipid hybrid nanoparticles: A novel drug delivery system for enhancing the activity of Psoralen against breast cancer
Publication date: 20 April 2019Source: International Journal of Pharmaceutics, Volume 561Author(s): Manling Du, Yong Ouyang, Fansu Meng, Xingwang Zhang, Qianqian Ma, Yong Zhuang, Hui Liu, Mujuan Pang, Tiange Cai, Yu CaiAbstractA polymer-lipid hybrid nanocarrier was developed to encapsulate psoralen (PSO) to improve its water solubility and bioavailability. The effects of PSO-loaded polymer-lipid hybrid nanoparticles (PSO-PLNs) on breast cancer MCF-7 cells were investigated. PSO-PLNs were prepared through a nanoprecipitation method and were optimized by a central composite design-response surface methodology using particle ...
Source: International Journal of Pharmaceutics - March 13, 2019 Category: Drugs & Pharmacology Source Type: research

An in vitro approach for evaluating the oral abuse deterrence of solid oral extended-release opioids with properties intended to deter abuse via chewing
Publication date: Available online 9 March 2019Source: International Journal of PharmaceuticsAuthor(s): Anna Externbrink, Satish Sharan, Dajun Sun, Wenlei Jiang, David Keire, Xiaoming XuAbstractThe introduction of prescription opioids with abuse-deterrent (AD) properties to the marketplace has created a need for new testing methodologies to evaluate the performance of potentially abuse-deterrent opioid products. Drug abusers may attempt to chew solid oral extended-release (ER) opioids prior to ingestion to bypass the ER mechanism of the formulation to achieve euphoria. In the present study, a chewing apparatus was utilized...
Source: International Journal of Pharmaceutics - March 10, 2019 Category: Drugs & Pharmacology Source Type: research

Preparation of cubic-shaped sorafenib-loaded nanocomposite using well-defined poly(vinyl alcohol alt-propenylene) copolymer
Publication date: Available online 10 March 2019Source: International Journal of PharmaceuticsAuthor(s): Tivadar Feczkó, Gabriella Merza, György Babos, Bernadett Varga, Eszter Gyetvai, László Trif, Ervin Kovács, Robert TubaAbstractVinyl alcohol (VA) copolymers having fine tunable polarities are emerging materials in drug delivery applications. VA copolymers rendering well-defined molecular architecture (C/OH ratio = 2, 4, 5 and 8) were used as carriers for model drug compound, fluorescein exhibited significantly different release characteristics depending on the polarity of the polymers. Ba...
Source: International Journal of Pharmaceutics - March 10, 2019 Category: Drugs & Pharmacology Source Type: research

Cytoplasmic Delivery of Functional siRNA Using pH-Responsive Nanoscale Hydrogels
Publication date: Available online 8 March 2019Source: International Journal of PharmaceuticsAuthor(s): William B. Liechty, Rebekah L. Scheuerle, Julia E. Vela Ramirez, Nicholas A. PeppasAbstractThe progress of short interfering RNA (siRNA) technologies has unlocked the development of novel alternatives for the treatment of a myriad of diseases, including viral infections, autoimmune disorders, or cancer. Nevertheless, the clinical use of these therapies faces significant challenges, mainly overcoming the charged and large nature of these molecules to effectively enter the cell. In this work, we developed a cationic polyme...
Source: International Journal of Pharmaceutics - March 9, 2019 Category: Drugs & Pharmacology Source Type: research

Influence of Mechanical and Thermal Energy on Nifedipine Amorphous Solid Dispersions Prepared by Hot Melt Extrusion: Preparation and Physical Stability
Publication date: Available online 8 March 2019Source: International Journal of PharmaceuticsAuthor(s): Xiangyu Ma, Siyuan Huang, Michael B. Lowinger, Xu Liu, Xingyu Lu, Yongchao Su, Robert O. WilliamsAbstractHot melt extrusion (HME) has been used to prepare solid dispersions, especially molecularly dispersed amorphous solid dispersions (ASDs) for solubility enhancement purposes. The energy generated by the extruder in the form of mechanical and thermal output enables the dispersion and dissolution of crystalline drugs in polymeric carriers. However, the impact of this thermal and mechanical energy on ASD systems remains u...
Source: International Journal of Pharmaceutics - March 9, 2019 Category: Drugs & Pharmacology Source Type: research

Spatiotemporal release of VEGF from biodegradable polylactic-co-glycolic acid microspheres induces angiogenesis in chick chorionic allantoic membrane assay
Publication date: Available online 8 March 2019Source: International Journal of PharmaceuticsAuthor(s): Omar Qutachi, Anthony J. Bullock, Giulia Gigliobianco, Sheila MacNeilAbstractWhile vascular endothelial growth factor (VEGF) is an acknowledged potent pro-angiogenic agent there is a need to deliver it at an appropriate concentration for several days to achieve angiogenesis. The aim of this study was to produce microspheres of biodegradable polylactic-co-glycolic acid (PLGA) tailored to achieve sustained release of VEGF at an appropriate concentration over seven days, avoiding excessive unregulated release of VEGF that h...
Source: International Journal of Pharmaceutics - March 9, 2019 Category: Drugs & Pharmacology Source Type: research

smartPearls® for dermal bioavailability enhancement – long-term stabilization of suspensions by viscoelasticity
Publication date: Available online 8 March 2019Source: International Journal of PharmaceuticsAuthor(s): David Hespeler, Daniel Knoth, M. Cornelia Keck, H. Rainer Müller, Sung Min PyoAbstractsmartPearls® are a novel dermal delivery system based on mesoporous (pores 2-50 nm) particles, developed in 2014. Their pores can be loaded with active which is long-term stabilized in its amorphous state. The increased saturation solubility by the amorphous state leads to an increased dermal bioavailability of poorly soluble actives. To avoid sedimentation of the porous particles (3-50 µm) in dermal formulations, viscoel...
Source: International Journal of Pharmaceutics - March 9, 2019 Category: Drugs & Pharmacology Source Type: research

Enzymatic Crosslinked Gelatin 3D Scaffolds for Bone Tissue Engineering
Publication date: Available online 8 March 2019Source: International Journal of PharmaceuticsAuthor(s): Mari Carmen Echave, Carolina Pimenta-Lopes, José Luis Pedraz, Mehdi Mehrali, Alireza Dolatshahi-Pirouz, Fransesc Ventura, Gorka OriveAbstractBone tissue engineering is an emerging medical field that has been developed in recent years to address pathologies with limited ability of bones to regenerate. Here we report the fabrication and characterization of microbial transglutaminase crosslinked gelatin-based scaffolds designed for serving as both cell substrate and growth factor release system. In particular, morpho...
Source: International Journal of Pharmaceutics - March 9, 2019 Category: Drugs & Pharmacology Source Type: research

Natural biodegradable polymers based nano-formulations for drug delivery: A review
Publication date: Available online 6 March 2019Source: International Journal of PharmaceuticsAuthor(s): Archana George, Priyanka A. Shah, Pranav S. ShrivastavAbstractNanomedicines are now considered as the new-generation medication in the current era mainly because of their features related to nano size. The efficacy of many drugs in their micro/macro formulations is shown to have poor bioavailability and pharmacokinetics after oral administration. To overcome this predicament, use of natural/synthetic biodegradable polymeric nanoparticles (NPs) have gained prominence in the field of nanomedicine for targeted drug delivery...
Source: International Journal of Pharmaceutics - March 7, 2019 Category: Drugs & Pharmacology Source Type: research

Formulation and Performance of Irbesartan Nanocrystalline Suspensions and Granulated or Bead-Layered Dried Powders- Part I
The objectives of the study were to formulate Irbesartan nanocrystalline suspensions via media milling, study the effects of process and formulation variables on particle size reduction, and evaluate bead layering or spray granulation as drying processes. A Design of Experiment approach was utilized to understand the impact of formulation variables on particle size reduction via media milling. Drug concentration and type of stabilizer were found to be significant in particle size reduction. Optimized Irbesartan nanocrystalline suspension (i.e. at 10% w/w with 1% w/w poloxamer 407) showed superior in vitro dissolution profi...
Source: International Journal of Pharmaceutics - March 7, 2019 Category: Drugs & Pharmacology Source Type: research

Managing API raw material variability during continuous twin-screw wet granulation
In this study, the impact of the raw material variability of an active pharmaceutical ingredient (API) in a high dose formulation on the twin-screw wet granulation process and on the resulting granule quality attributes was investigated. In a previous study (Stauffer et al., 2018), eight API batches were characterized to determine the API batch-to-batch variability. Principal component analysis (PCA) was then used to analyse the raw material property differences between the API batches and to determine the causes of the batch-to-batch variability. In current study, the three principal components from that PCA model were us...
Source: International Journal of Pharmaceutics - March 7, 2019 Category: Drugs & Pharmacology Source Type: research

Polymer–lipid hybrid nanoparticles: a novel drug delivery system for enhancing the activity of Psoralen against breast cancer
Publication date: Available online 6 March 2019Source: International Journal of PharmaceuticsAuthor(s): Manling Du, Yong Ouyang, Fansu Meng, Xingwang Zhang, Qianqian Ma, Yong Zhuang, Hui Liu, Mujuan Pang, Tiange Cai, Yu CaiAbstractA polymer–lipid hybrid nanocarrier was developed to encapsulate psoralen (PSO) to improve its water solubility and bioavailability. The effects of PSO–loaded polymer–lipid hybrid nanoparticles (PSO-PLNs) on breast cancer MCF-7 cells were investigated. PSO-PLNs were prepared through a nanoprecipitation method and were optimized by a central composite design-response surface metho...
Source: International Journal of Pharmaceutics - March 7, 2019 Category: Drugs & Pharmacology Source Type: research

Effects of Conductive Polyazulene and Plasticizer Embedded in Deproteinized Natural Rubber Transdermal Patch on Electrically Controlled Naproxen Release-Permeation
Publication date: Available online 6 March 2019Source: International Journal of PharmaceuticsAuthor(s): Rattanapond Kaewchingduang, Nophawan Paradee, Anuvat Sirivat, Sumonman NiamlangAbstractNaproxen (Npx) was utilized as an anionic drug and loaded in the deproteinized natural rubber (DPNR) films prepared by the UV irradiation. The in-vitro drug release-permeation from the DPNR films and through the pig skin was investigated under the effects of the plasticizer type and amount, silicone oil (Si) and dibutyl phthalate (DBP), applied electric potential, and used conductive polyazulene as the drug encapsulation host. The drug...
Source: International Journal of Pharmaceutics - March 7, 2019 Category: Drugs & Pharmacology Source Type: research

Influence of emulsifier concentration on partition behavior and chemical stability of betamethasone dipropionate in emulsion gels
Publication date: Available online 6 March 2019Source: International Journal of PharmaceuticsAuthor(s): Julia Puschmann, Michael E. Herbig, Christel C. Müller-GoymannAbstractThe partitioning of active pharmaceutical ingredients (API) in emulsions is influenced by various factors, such as composition of the phases, emulsifier type and concentration, and temperature. Therefore, the chemical stability of the API can be influenced by its partitioning into the aqueous phase as degradation is typically facilitated in water. With increasing emulsifier concentration from 0.15% to 5.0%, more betamethasone dipropionate (BDP) wa...
Source: International Journal of Pharmaceutics - March 7, 2019 Category: Drugs & Pharmacology Source Type: research

Cytotoxicity and Permeability Enhancement of Capmul®MCM in Nanoemulsion Formulation
This study aimed to investigate the following factors affecting the cytotoxicity of Capmul®MCM (C8/10MD) in self-emulsified nanoemulsions (SENs): concentration, triglycerides, and droplet size, and how these factors influence permeability of lipid droplets. Two triglycerides (C8T and C18T) and six formulations were used: SEN1(C18T:C8/10MD:Kolliphor®RH40=7:3:10, 257 nm), SEN2(C8T:C8/10MD:Kolliphor®RH40=1:1:2, 30 nm), SEN3(C18T:Kolliphor®RH40=1:4, 26 nm), SEN4(C8T:Kolliphor®RH40=1:4, 27 nm), SEN5(C8/10MD:Kolliphor®RH40=1:1, 120 nm) and SEN6(C8/10MD:Kolliphor®RH40=1:4, 15 nm). There was no cytotoxi...
Source: International Journal of Pharmaceutics - March 7, 2019 Category: Drugs & Pharmacology Source Type: research

Self-Assembled Tannic Acid Complexes for pH-Responsive Delivery of Antibiotics: Role of Drug-Carrier Interactions
Publication date: Available online 7 March 2019Source: International Journal of PharmaceuticsAuthor(s): Sara A. Abouelmagd, Noura H. Abd Ellah, Omar Amen, Alshaimaa Abdelmoez, Noha G. MohamedAbstractSelf-assembled particles, based on non-covalent interactions, are attractive drug carriers with a relatively simple structure and easy preparation. Tannic acid (TA) is an anionic polyphenolic compound with a wide range of molecular interactions and diverse applications in drug delivery research. Here, we propose the use of TA complexes with cationic antibiotics as a new pH-responsive drug carriers of high drug loading and optim...
Source: International Journal of Pharmaceutics - March 7, 2019 Category: Drugs & Pharmacology Source Type: research

Corona Alternating Current Electrospinning: A combined approach for increasing the productivity of electrospinning
Publication date: Available online 4 March 2019Source: International Journal of PharmaceuticsAuthor(s): Balázs Farkas, Attila Balogh, Richárd Cselkó, Kolos Molnár, Attila Farkas, Enikő Borbás, György Marosi, Zsombor Kristóf NagyAbstractCorona alternating current electrospinning (C-ACES), a scaled-up productivity electrospinning method was developed by combining the intense forces of the alternating electrostatic field and a sharp-edged spinneret design with increased free surface. C-ACES reached two orders of magnitude higher productivity (up to 1,200 mL/h) than the clas...
Source: International Journal of Pharmaceutics - March 6, 2019 Category: Drugs & Pharmacology Source Type: research

Direct and Simultaneous Determination of Intra-liposomal and External Sulfate in Liposomal Doxorubicin Formulations by Capillary Electrophoresis / Inductively Coupled Plasma - Tandem Mass Spectrometry (CE/ICP-MS/MS)
Publication date: Available online 4 March 2019Source: International Journal of PharmaceuticsAuthor(s): Siyam M. Ansar, Thilak MudaligeAbstractA capillary electrophoresis coupled to an inductively coupled plasma – tandem mass spectrometry (CE/ICP-MS/MS) method was developed and validated for the determination of external and intra-liposomal sulfate in doxorubicin liposomal formulations. Ammonium sulfate is a critical component of liposomes, in the loading and maintenance of drug in the intraliposomal space. Complete separation of external and intra-liposomal sulfate was achieved using CE with minimal liposome disrupt...
Source: International Journal of Pharmaceutics - March 6, 2019 Category: Drugs & Pharmacology Source Type: research

A Design of Experiment (DoE) approach to optimise spray drying process conditions for the production of trehalose/leucine formulations with application in pulmonary delivery
Publication date: Available online 5 March 2019Source: International Journal of PharmaceuticsAuthor(s): S. Focaroli, P.T. Mah, J.E. Hastedt, I. Gitlin, S. Oscarson, J.V. Fahy, A.M. HealyAbstractThe present study evaluates the effect of L-leucine concentration and operating parameters of a laboratory spray dryer on characteristics of trehalose dry powders, with the goal of optimizing production of these powders for inhaled drug delivery. Trehalose/L-leucine mixtures were spray dried from aqueous solution using a laboratory spray dryer. A factorial design of experiment (DoE) was undertaken and process parameters adjusted wer...
Source: International Journal of Pharmaceutics - March 6, 2019 Category: Drugs & Pharmacology Source Type: research