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Wednesday, November 9, 2016

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Wednesday, November 2, 2016

Highlighted Article: Evaluation of Eudragit® Retard Polymers for the Microencapsulation of Alpha-Lipoic Acid



Evaluation of Eudragit® Retard Polymers for the Microencapsulation of Alpha-Lipoic Acid


Author(s):

Tiziana M.G. Pecora, Teresa Musumeci, Lucrezia Musumeci, Massimo Fresta and Rosario Pignatello   Pages 1165 - 1175 ( 11 )

Abstract:


Background: Microencapsulation of natural antioxidants in polymeric systems represents a possible strategy for improving the oral bioavailability of compounds that are otherwise poorly soluble.
Objective: α-lipoic acid (ALA) was microencapsulated with polymethacrylate polymers (blends at various ratios of Eudragit® RS100 and RL100 resins).
Method: Microspheres were produced by solvent displacement of an ethanol cosolution of ALA and polymers; the microsuspensions were then freeze-dried, using trehalose as a cryoprotector. Microspheres were characterized in the solid state for micromeritic properties and drug loading, as well as by infrared spectroscopy, powder X-ray diffractometry and differential scanning calorimetry. The antioxidant activity of free and encapsulated ALA was assessed by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay.
Results: In vitro release studies, performed in simulated gastric (pH 1.2) and intestinal fluid (pH 6.8), showed that, depending on polymer composition and drug-to-polymer ratio, ALA release can be slowed down, compared to the dissolution pattern of the free drug. Solid-state characterization confirmed the chemical stability of ALA in the microspheres, suggesting that ALA did not develop strong interactions with the polymer and was present in an amorphous or a disordered-crystalline state within the polymer network. As indicated by the DPPH assay, the microencapsulation of ALA in Eudragit® Retard matrices did not alter its antioxidant activity.
Conclusion: ALA was effectively encapsulated in Eudragit® Retard matrices, showing a chemical stability up to 6 months at room conditions and at 40°C. Moreover, since the drug maintained its antioxidant activity in vitro, the potential application of these microparticulate systems for oral administration would deserve further studies.

Keywords:

Antioxidant activity, coevaporates, DPPH assay, Eudragit® Retard, lipoic acid, microencapsulation, polymers.

Affiliation:

Department of Drug Sciences, University of Catania, Viale A. Doria, 6; I-95125 Catania, Italy.

Graphical Abstract:





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Tuesday, October 25, 2016

Most Accessed Article: The Controlled Release of Drugs and Bioactive Compounds from Mesoporous Silica Nanoparticles


The Controlled Release of Drugs and Bioactive Compounds from Mesoporous Silica Nanoparticles

Author(s):

Mohammad A. ChowdhuryPages 839-856 (18)

Abstract:


In recent period of time the mesoporous silica nanoparticles (MSNs) have been extensively utilised in controlled release (CR) applications. This burgeoning research is favoured because of the unique characteristics of the MSNs such as, ordered and homogenous pore network, high surface area and pore volumes, silanol-containing surfaces, and relatively low toxic in nature. However, for an effective targeted drug delivery, these materials offer numerous challenges such as, to reduce the complications and toxicity and avoid any undesired interactions of the MSNs with the untargeted healthy cells and membranes. A range of concepts and techniques have been implied to overcome these challenges. This article presents an overview on the recent research advancements in CR of drugs and bioactive compounds from the MSNs. Based on the past researches that took place over the last 15 years, the article illustrates three particular areas: 1) unmodified MSNs, 2) modified MSNs, and 3) biocompatibility, bio-toxicity, tissue responses and cellular uptakes of the MSNs. The three encompassed areas of research describe enormous diversities and complexities which span the aspects of complex designs and syntheses, types of silica materials being used, drug loadings, types of drug used, and ranges of biological evaluations of the MSNs. Perspectives and insights are presented into a range of aspects such as, syntheses, characterisations, functionalisation and incorporations of biomacromolecules into the MSNs; drug loadings and drug release kinetics; biological evaluations such as, biocompatibility, bio-toxicity and intracellular drug delivery; and, the effects of size, shape, morphology, structural and textural properties of the MSNs.

Keywords:

Bioactive compound, biopolymer, cell, drug, mesoporous, nanoparticles, silica, tissue, toxicity.

Affiliation:

School of Chemistry, Monash University, Wellington Road, Clayton 3800, Melbourne, Australia.

Graphical Abstract:






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Wednesday, October 19, 2016

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Wednesday, October 5, 2016

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Highlighted Article Flyer for the journal “Current Drug Delivery” Volume 13, Number 3



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Current Drug Delivery :::: New Issue



Current Drug Delivery aims to publish peer-reviewed articles, research articles, short and in-depth reviews, and drug clinical trials studies in the rapidly developing field of drug delivery. Modern drug research aims to build delivery properties of a drug at the design phase, however in many cases this idea cannot be met and the development of delivery systems becomes as important as the development of the drugs themselves.The journal is essential for all pharmaceutical scientists involved in drug design, development and delivery.
Following are the articles from the journal Current Drug Delivery, Volume 12 Issue 4: 
Immunostimulant Properties of Chemical Delivery Systems in Vaccine Development
Author(s): Sahar Hosseinzadeh and Azam Bolhassani


Chitosan: A Propitious Biopolymer for Drug Delivery
Author(s): Dibyangana S. Duttagupta, Varsha M. Jadhav and Vilasrao J. Kadam

Novel Delivery Systems for Anti-Allergic Agents: Allergic Disease and Innovative Treatments  
Author(s)Carla M. Lopes, Pedro B. Coelho and Rita Oliveira

Preparation, characterization and in vitro release of zein-pectin capsules for target delivery
Author(s)Wai-Wa Tang, Fangyuan Dong, Ka-Hing Wong and Yi Wang

Biochemical Characterization of GM1 Micelles-Amphotericin B Interaction
Author(s)Victoria Leonhard, Roxana V. Alasino, Ismael D. Bianco, Ariel G. Garro, Valeria Heredia and Dante M. Beltramo

Physically Cross-linked Hydrogels of β -cyclodextrin Polymer and Poly(ethylene glycol)-cholesterol as Delivery Systems for Macromolecules and Small Drug Molecules 
Author(s)Shaaban K. Osman, Ghareb M. Soliman and Saleh Abd El Rasoul

Formulation and Evaluation of Different Floating Tablets Containing Metronidazole to Target Stomach
Author(s): Zhiao C. Loh and Amal A. Elkordy

Production of β -cyclodextrin from pH and Thermo Stable Cyclodextrin Glycosyl Transferase, Obtained from Arthrobacter mysorens and Its Evaluation as a Drug Carrier for Irbesartan
Author(s): Y. Rajesh, K. Narayanan, M. Sreenivasa Reddy, Vijaya K. Bhaskar, G. Gautham Shenoy, V. M. Subrahmanyam and J. Venkata Rao

Boswellia carterii Liquisolid Systems with Promoted Anti-inflammatory Activity
Author(s): Dina Mahmoud Mostafa, Nagwa Mohammed Ammar, Sameh Hosam Abd El-Alim, Ahmed Alaa Kassem, Rehab Ali Hussein, Gamal Awad and Sally Abdul-Wanees El-Awdan

Development and Characterization of Spray Dried Microparticles for Pulmonary Delivery of Antifungal Drug
Author(s)Divita Mathpal, Tarun Garg, Goutam Rath and Amit Kumar Goyal

For details, please visit: http://bit.ly/1Edepe4
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Articles from Bentham Science Impact Factor Journal ‘Current Drug Delivery’



Current Drug Delivery aims to publish peer-reviewed articles, research articles, short and in-depth reviews, and drug clinical trials studies in the rapidly developing field of drug delivery. Modern drug research aims to build delivery properties of a drug at the design phase, however in many cases this idea cannot be met and the development of delivery systems becomes as important as the development of the drugs themselves. The journal aims to cover the latest outstanding developments in drug and vaccine delivery employing physical, physico-chemical and chemical methods. The drugs include a wide range of bioactive compounds from simple pharmaceuticals to peptides, proteins, nucleotides, nucleosides and sugars. The journal will also report progress in the fields of transport routes and mechanisms including efflux proteins and multi-drug resistance. The journal is essential for all pharmaceutical scientists involved in drug design, development and delivery.

Articles from the journal Current Drug Delivery

Author(s): Sahar Hosseinzadeh and Azam Bolhassani

Author(s): Dibyangana S. Duttagupta, Varsha M. Jadhav and Vilasrao J. Kadam


Author(s): Carla M. Lopes, Pedro B. Coelho and Rita Oliveira

Author(s): Wai-Wa Tang, Fangyuan Dong, Ka-Hing Wong and Yi Wang

Author(s): Victoria Leonhard, Roxana V. Alasino, Ismael D. Bianco, Ariel G. Garro, Valeria Heredia and Dante M. Beltramo

Author(s): Shaaban K. Osman, Ghareb M. Soliman and Saleh Abd El Rasoul

Author(s): Zhiao C. Loh and Amal A. Elkordy

Author(s): Y. Rajesh, K. Narayanan, M. Sreenivasa Reddy, Vijaya K. Bhaskar, G. Gautham Shenoy, V. M. Subrahmanyam and J. Venkata Rao

Author(s): Dina Mahmoud Mostafa, Nagwa Mohammed Ammar, Sameh Hosam Abd El-Alim, Ahmed Alaa Kassem, Rehab Ali Hussein, Gamal Awad and Sally Abdul-Wanees El-Awdan

Author(s): Divita Mathpal, Tarun Garg, Goutam Rath and Amit Kumar Goyal

courtesy by : https://benthamsciencepublishers.wordpress.com/2015/08/28/articles-from-bentham-science-impact-factor-journal-current-drug-delivery/

Recently Published Issue of the Journal Current Drug Delivery



Current Drug Delivery aims to publish peer-reviewed articles, research articles, short and in-depth reviews, and drug clinical trials studies in the rapidly developing field of drug delivery. Modern drug research aims to build delivery properties of a drug at the design phase, however in many cases this idea cannot be met and the development of delivery systems becomes as important as the development of the drugs themselves.The journal is essential for all pharmaceutical scientists involved in drug design, development and delivery.
Following are the articles from the Journal of Current Drug Delivery, 12 Issue 3:
Article: Current Approaches for in vitro Drug Release Study of Long Acting Parenteral Formulations
Author(s): Tejas M. Dadhaniya, Om Prakash Sharma, Mukesh C. Gohel and Priti J. Mehta

Article: Nanodiamonds as a New Horizon for Pharmaceutical and Biomedical Applications
Author(s): Harsiddhi M. Chaudhary, Aindrilla S. Duttagupta, Kisan R. Jadhav, Sai V. Chilajwar and Vilasrao J. Kadam

Article: Disulphide-Thiol Chemistry: A Multi-Faceted Tool for Macromolecular Design and Synthesis of Polyfunctional Materials for Specialized Drug Delivery
Author(s): Teboho Kgesa, Yahya E. Choonara, Charu Tyagi, Lomas K. Tomar, Pradeep Kumar, Lisa C. du Toit and Viness Pillay

Article: Probiotic and Prebiotic-probiotic PEC Microparticles for Sustaining and Enhancing Intestinal Probiotic Growth
Article: K. Harshitha, P. K. Kulkarni, Rudra Vaghela, V. Naga Sravan Kumar Varma, D. Rohan Deshpande and Umme Hani

Article: The in vitro and in vivo Evaluation of Fenofibrate with a Self- Microemulsifying Formulation
Author(s): L i Xiumin, G e Man, L u Minzi, Jin Yinghua and Quan Dongqin

Article: Preparation and Evaluation of Multi Particulates Drug Delivery System Using Natural Polymers
Author(s): Tariq Baig, Hammad Sheikh, Ankur Srivastava, Pushpendra K. Tripathi and Shalini Tripathi

Article: Transmucosal Delivery of Linagliptin for the Treatment of Type- 2 Diabetes Mellitus by Ultra-Thin Nanofibers
Author(s): Vedant Modgill, Tarun Garg, Amit K. Goyal and Goutam Rath

Article: Gemcitabine Interacts with Carbonate Apatite with Concomitant Reduction in Particle Diameter and Enhancement of Cytotoxicity in Breast Cancer Cells
Author(s): Fitya S. Mozar and Ezharul H. Chowdhury

Article: The Role of Tomatine Adjuvant in Antigen Delivery for Cross- Presentation
Author(s): Paul Y.-J. Hsu, Ching-An Wu, Shan-Shan Shen and Ya-Wun Yang

Article: Characterization of Novel Composite Alginate Chitosan-Carrageenan Nanoparticles for Encapsulation of BSA as a Model Drug Delivery System
Author(s): Landi Cheng, Cody Bulmer and Argyrios Margaritis

For details, please visit: http://bit.ly/1FlOU9n

courtesy by : https://benthamsciencepublishers.wordpress.com/2015/07/13/recently-published-issue-of-the-journal-current-drug-delivery-3/

Current Drug Delivery , 13 Issue 6



Current Drug Delivery aims to publish peer-reviewed articles, research articles, short and in-depth reviews, and drug clinical trials studies in the rapidly developing field of drug delivery. Modern drug research aims to build delivery properties of a drug at the design phase, however in many cases this idea cannot be met and the development of delivery systems becomes as important as the development of the drugs themselves.
The journal aims to cover the latest outstanding developments in drug and vaccine delivery employing physical, physico-chemical and chemical methods. The drugs include a wide range of bioactive compounds from simple pharmaceuticals to peptides, proteins, nucleotides, nucleosides and sugars. The journal will also report progress in the fields of transport routes and mechanisms including efflux proteins and multi-drug resistance.
The journal is essential for all pharmaceutical scientists involved in drug design, development and delivery.

Articles from the journal Current Drug Delivery , 13 Issue 6

For details on the articles, please visit this link :: http://bit.ly/2bkkMci
courtesy by : https://benthamsciencepublishers.wordpress.com/2016/09/12/new-issue-current-drug-delivery-13-issue-6/

Monday, July 25, 2016

Pharmacogenetics of Intestinal Absorption

Author(s):

Tsutomu Nakamura, Motohiro Yamamori and Toshiyuki SakaedaPages 153-169 (17)

Abstract:


The small intestine is the primary site of absorption for many drugs administered orally and so is the target tissue for pharmacotherapeutic strategies to control the oral absorption of drugs. Drug transporters, including the ATP-binding cassette (ABC) superfamily and the solute carrier (SLC) superfamily, have been considered to play a physiological role in regulating the absorption of xenobiotics, and variations in their expression level and function in the small intestine cause intra- and inter-individual variation in the oral absorption of drugs. Recent advances in molecular biology have suggested that genetic polymorphisms are associated with the expression level and function, and thereby inter-individual variation. In this review, the pharmacogenetics of these transporters is summarized, and their future significance in the clinical setting is discussed.

Affiliation:

Department of Clinical Evaluation of Pharmacotherapy, Kobe University Graduate School of Medicine,Kobe 650-0047, Japan.


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Enhanced Delivery of Topically-Applied Formulations Following Skin Pre-Treatment with a Hand-Applied, Plastic Microneedle Array

Author(s):

Dan Duan, Craig Moeckly, Jerry Gysbers, Chris Novak, Gayatri Prochnow, Kris Siebenaler, Leila Albers and Kris HansenPages 557-565 (9)

Abstract:


The purpose of this work is to characterize microchannels created by polymeric microneedles, applied by hand, and to demonstrate enhanced delivery of topically applied formulations of lidocaine hydrochloride and methylprednisolone sodium succinate (MPSS). 3Ms Microstructured Transdermal System (MTS) arrays were applied to domestic swine to demonstrate reliability of penetration, depth of penetration and durability of the structures to repeat application and high force. Tissue levels of lidocaine and MPSS following topical application with and without microneedle pretreatment were determined by HPLC-MS analysis following digestion of biopsies. Almost all microneedles penetrate the stratum corneum upon hand force application. The depth of penetration varies from < 100μm to nearly 150μm depending on the application force and the firmness of the underlying tissue. The arrays show excellent durability to repeated in-vivo application, with less than 5% of the structures evidencing even minimal tip bending after 16 applications. Under extreme force against a rigid surface, the microneedles bend but do not break. A lidocaine hydrochloride formulation applied topically in-vivo showed ∼340% increase in local tissue levels when the MTS arrays were used to twice pre-treat the skin prior to applying the drug. Local delivery of a topically applied formulation of MPSS was over one order of magnitude higher when the application site was twice pre-treated with the MTS array. 3Ms MTS array (marketed as 3M™ Microchannel Skin System) provides repeatable and robust penetration of the stratum corneum and epidermis and enhances delivery of some formulations such as lidocaine hydrochloride.

Keywords:

Dermis, epidermis, stratum corneum penetration, microneedles, microporation, dermal, stratum corneum, lidocaine, absorption, drug delivery, transdermal, skin

Affiliation:

3M Drug Delivery Systems Division, Building 260-03-A-05, St. Paul MN 55114, USA.


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Anatomical and Histological Factors Affecting Intranasal Drug and Vaccine Delivery

Author(s):

Sveinbjorn GizurarsonPages 566-582 (17)

Abstract:


The aim of this review is to provide an understanding of the anatomical and histological structure of the nasal cavity, which is important for nasal drug and vaccine delivery as well as the development of new devices. The surface area of the nasal cavity is about 160 cm2, or 96 m2 if the microvilli are included. The olfactory region, however, is only about 5 cm2 (0.3 m2 including the microvilli). There are 6 arterial branches that serve the nasal cavity, making this region a very attractive route for drug administration. The blood flow into the nasal region is slightly more than reabsorbed back into the nasal veins, but the excess will drain into the lymph vessels, making this region a very attractive route for vaccine delivery. Many of the side effects seen following intranasal administration are caused by some of the 6 nerves that serve the nasal cavity. The 5th cranial nerve (trigeminus nerve) is responsible for sensing pain and irritation following nasal administration but the 7th cranial nerve (facial nerve) will respond to such irritation by stimulating glands and cause facial expressions in the subject. The first cranial nerve (olfactory nerve), however, is the target when direct absorption into the brain is the goal, since this is the only site in our body where the central nervous system is directly expressed on the mucosal surface. The nasal mucosa contains 7 cell types and 4 types of glands. Four types of cells and 2 types of glands are located in the respiratory region but 6 cell types and 2 types of glands are found in the olfactory region.

Keywords:

Drug delivery, intranasal administration, nasal administration, nasal anatomy, nasal cavity, nasal device, nasal histology, vaccine delivery

Affiliation:

Faculty of Pharmaceutical Sciences, University of Iceland, Hofsvallagata 53, 107 Reykjavik, Iceland.


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Temporal Separation in the Release of Bioactive Molecules from a Moldable Calcium Sulfate Bone Graft Substitute

Author(s):

Matt E. Brown, Yuan Zou, R. Peyyala, Thomas D. Dziubla and David A. PuleoPages 605-612 (8)

Abstract:


Treatment of infected bone defects presents a considerable challenge due to the complications that occur from significant bone damage concomitant with contaminated tissue. These wounds are most often treated in a two-step sequence, where the infection is first eliminated before any attempt to repair the bone is undertaken. In order to combine these two treatment steps into one procedure, a moldable bone grafting material was developed to deliver drugs in a temporally separated manner. This was accomplished by a two-layered calcium sulfate composite consisting of a moldable outer shell containing antibiotic-loaded poly(lactic-co-glycolic acid) microspheres wrapped around a preformed core containing an osteogenic drug. The release of vancomycin from the shell portion began immediately and continued over the course of 6 weeks, while the release of simvastatin from the core was delayed for 12 days before being released over the next 4 weeks. Bioactivity of vancomycin was shown in modified Kirby-Bauer experiments in which whole samples inhibited Staphylococcus aureus (S. aureus) growth for 2 weeks. This two-layered system is capable of delivering antibiotics locally for clinically relevant periods of time and delaying the release of osteogenic drugs to mimic a two-step procedure that has potential for treating infected bone defects.

Keywords:

Bone filler, bone graft substitute, calcium sulfate, composite, moldable, sequential release, simvastatin, vancomycin.

Affiliation:

522A Robotics and Manufacturing Building, Department of Biomedical Engineering, University of Kentucky, Lexington, KY 40506-0108, USA.

Graphical Abstract:



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