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Current Drug Delivery

Rawda Yaseen AlSheyyab, Bashar Mohammad Al-Taani, Rana Mohammad Obeidat, Motasem Mohammad Alsmadi, Rafeef Khalid Masaedeh, Raghda Nasry Sabat
GnRH antagonists have several clinical applications in prostate cancer, regulation of ovulation induction in females, breast cancer, male contraception and others. Antagonists differ from natural GnRH decapeptide in having five or more amino acid substitutions. Whereas most of antagonists are available as subcutaneous (SC) formula for injection, some are formulated as a depot formulation for sustained release (e.g. Cetrarelix, Degarelix). Systemic delivery of cetrorelix acetate by intratracheal route can be achieved using dry powder for inhalation of adhesive mixture when the powder deposition reaches stage four...
February 14, 2018: Current Drug Delivery
Shymaa Hatem, Maha Nasr, Seham A Elkheshen, Ahmed S Geneidi
Antioxidants are among the most important cosmeceuticals, with proven ability of inhibiting cellular damage. The topical skin administration of antioxidants is essential for minimizing skin aging and achieving better skin protection against harmful free radicals. However, their unfavorable physiochemical properties such as chemical instability, excessive hydrophilicity or lipophilicity and others could be a great obstacle against their skin promising effects as well as their delivery to deeper skin layers. These problems could all be remedied through the use of delivery carriers...
February 14, 2018: Current Drug Delivery
Nadine Schaefer, Ann-Katrin Kroll, Matthias W Laschke, Michael D Menger, Hans H Maurer, Markus R Meyer, Peter H Schmidt
BACKGROUND: Since their appearance on the drugs of abuse market, synthetic cannabinoids (SCs) are gaining increasing toxicological relevance. They are consumed without knowledge of their toxicokinetic (TK) and toxicodynamic properties and human studies are not allowed due to ethical reasons. A controlled animal TK study following nebulization of 4-ethylnaphthalene-1-yl-(1-pentylindole-3-yl)methanone (JWH-210), 2-(4-methoxyphenyl)-1-(1-pentyl-indole-3-yl)methanone (RCS-4) as well as Δ9-tetrahydrocannabinol (THC) to pigs should be helpful for better interpretation of analytical results in cases of misuse or poisoning...
February 14, 2018: Current Drug Delivery
Nandkishor S Talware, Remeth J Dias, V Rama Mohan Gupta
The imbalance of hydrophilicity, and lipophilicity along with, a large molecular size (due to a unique chemical structure) of natural compounds, or plant actives pose a significant challenge for their absorption through a biological membrane and thus, alters the therapeutic efficacy. Therefore, it is desirable to have a novel approach for such formulation in order to improve the solubility and bioavailability, of these phytoconstituents as a phospholipid complexation. Herbal drugs are precisely, embedded and bound by phospholipids to form vesicular structures, which are amphoteric in nature...
February 8, 2018: Current Drug Delivery
Hamed Vakilzadeh, Jaleh Varshosaz, Mohsen Minaiyan
INTRODUCTION: Triptorelin the synthetic analog of gonadotrophin-releasing hormone is used for treatment of sex hormone dependent diseases via parenteral administration. The aim of the present study was investigation the possibility of triptorelin pulmonary delivery and preparation of a pulmonary nanocarrier delivery system for it. METHODS: Triptorelin was loaded in Pluronic-F127 grafted poly (methyl vinyl ether-alt-maleic acid) nanomicelles by direct dissolution method...
February 8, 2018: Current Drug Delivery
Golnar Dorraj, Simin Dadashzadeh, Mohammad Erfan, Hamid Reza Moghimi
Nanoparticles (NPs) suffer from rapid clearance from body and require frequent dosing if long treatment is required. In order to solve this problem for solid lipid nanoparticles (SLN) and prolong their action, SLNs were incorporated into thermo-responsive Poloxamer sol-gels and their fate was investigated in-vivo and in-vitro using a near infrared lipophilic fluorescent dye; dialkylcarbocyanin (1). Leakage test, release of intact SLNs from sol-gel and SLN size and zeta potential were investigated. Biodistribution of DiR formulations (solution, free SLN and SLN-Gel) were investigated by whole-body and ex-vivo organ imaging after intraperitoneal injection in mice...
January 31, 2018: Current Drug Delivery
Na Chen, Run-Jun Xu, Li-Li Wang, Meng Zhang, Shi-Cheng Feng, Ju-Ying Zhou, Yu Tu
The effect of magnesium sulfate on brain tissue of SD rats irradiated by 6MeV electron was investigated. SD rats were divided into three groups: control group, irradiation (IR group) and irradiation treated with magnesium sulfate (IR+M group). After being anesthetized, the whole brains of IR group and IR+M group were exposed to 6 MeV electron radiation. IR+M group was i.p. injected with 10% magnesium sulfate (400 mg/kg) one day before radiation and three day, five days after radiation. And on the 1st, 3rd, 7th and 14th day after radiation, SD rats were euthanatized to take brain tissue for the detection of calcium, redox status and cell apoptosis, as well as the expression of NF-κB and ICAM-1...
January 23, 2018: Current Drug Delivery
Muhammad Zia Ullah Khan, Shujaat Ali Khan, Muhammad Ubaid, Aamna Shah, Rozina Kousar, Ghulam Murtaza
Androgenetic alopecia, generally recognized as male pattern baldness, is a gradually developing medical and physiological change, which is manifested by continuous hair-loss from scalp. Finasteride (4-aza-3-oxosteroid) is a potent anti-baldness compound that selectively and competitively inhibits the 5α-reductase isoenzymes. Prolonged oral use of finasteride leads to the emergence of sexual disorders including decrease in libido, gynecomastia, erectile dysfunction, ejaculation disorder, orgasm disorders and mood disturbances...
January 23, 2018: Current Drug Delivery
Akbar L Marzan, Rahnuma Tabassum, Basarat Jahan, Mehedi H Asif, Hasan M Reza, Mohsin Kazi, Sultan M Alshehri, Marcel de Matas, Mohammad H Shariare
BACKGROUND: Nano drug delivery systems have the potential to address the challenges of delivering BCS Class II and IV drugs like furosemide. The purpose of the current study is to prepare stable nanosuspension and investigate in vitro dissolution performance of the model compound furosemide using quality by design (QbD) approach. METHODS: Nanosuspension batches with uniform particle size were prepared for furosemide using the antisolvent precipitation method. A quality by design (Qbd) approach was explored to understand the impact of process parameters (stirring time, stirring speed, temperature, and injection rate) and material attributes (drug concentration, stabilizer type, drug: stabilizer ratio, and antisolvent: solvent ratio) on the quality attributes of furosemide nanosuspension using a full factorial experimental design...
January 22, 2018: Current Drug Delivery
Ahmed M Agiba, Maha Nasr, Sameh Abdel-Hamid, Ahmed B Eldin, Ahmed S Geneidi
Liposomes are promising systems for the delivery of macromolecules and poorly absorbed drugs, owing to their ability to compartmentalize drugs, their biodegradability and biocompatibility. The aim of the present study was to formulate and evaluate conventional and modified glucosamine sulphate (GluS) and chondroitin sulphate (CS) liposomal formulations, to enhance their oral permeation for treatment of osteoarthritis (OA). Liposomal formulations were prepared by the thin-film hydration method using two types of phospholipids; Epikuron 200© and Epikuron 200© SH, and three permeation enhancers; poloxamer 407, cetylpyridinium chloride, and sodium deoxycholate...
January 22, 2018: Current Drug Delivery
Michele Campos Alves, Priscila Aparecida de Almeida, Hudson Caetano Polonini, Carla Aparecida Pereira Bhering, Anderson de Oliveira Ferreira, Marcos Antonio Fernandes Brandao, Nadia Rezende Barbosa Raposo
BACKGROUND: Taxifolin (TAX) is a flavonoid that has numerous pharmacological properties, including an antioxidant ability superior to that of other flavonoids due to its particular structure. Nevertheless, it has low oral bioavailability, which limits its therapeutic application. In this context, potentially important approaches for systemic drug delivery could be by alternative routes such as skin and vaginal mucosa, once both routes have a variety of advantages compared with the oral route, including the ability to bypass both first-pass hepatic metabolism and the consequent degradation in the gastrointestinal tract...
January 15, 2018: Current Drug Delivery
Mohsin Kazi, Rayan Rayan Al Amri, Fars K Alanazi, Muhammad Delwar Hussain
A great number of new drug candidates identified from the discovery pipeline are poorly water soluble, which is a drawback to bring such candidates into the pharmaceutical market. Formulating these compounds as self-emulsifying/microemulsifying/ nanoemulsifying drug delivery systems (SEDDS/SMEDDS/SNEDDS) within lipid based formulations is of growing interests. Some of the recent studies have resulted in commercial products that provided improved bioavailability and dissolution due to the better dispersion properties of SEDDS/SMEDDS/SNEDDS...
January 15, 2018: Current Drug Delivery
Sanjoy Kumar Das, Soumalya Chakraborty, Chhandita Roy, Rajan Rajabalaya, Amal Widaad Mohaimin, Jasmina Khanam, Arunabha Nanda, Sheba R David
BACKGROUND: In the study of lipid vesicular carriers in permeation enhancement of drug molecules across skin after the success story of liposomes, ethosomes are a recent addition. There are a number of published reviews but still, there is a lack of reviews representing various aspects in a systematic way with a detailed description of current research works. This review serves to fill this deficiency along with a special emphasize on its preparation methods and application. METHODS: Information was collected from previously published literatures which were represented after analysis in terms of various aspects such as principles, composition, preparation, mechanism of penetration, modified forms, characterization, marketed preparation and its application...
January 15, 2018: Current Drug Delivery
Attila Leber, Maria Budai-Szucs, Edit Urban, Peter Valyi, Anita Kovacs, Szilvia Berko, Erzsebet Csanyi
BACKGROUND: Periodontitis is a chronic inflammatory disease, which affects the supporting tissues of the teeth, and without proper treatment it may lead to tooth loss. Antibiotics - dministered orally - have been widely used in the treatment of periodontitis. With the conventional administration routes, adequate drug levels cannot be reached in the periodontal pockets and oral application of antimicrobials could lead to side effects. Drug delivery systems containing antibiotics, administered at the site of infection, could possibly help eliminate pathogen bacteria and treat periodontitis...
January 15, 2018: Current Drug Delivery
Flavia De Marco Almeida, Carolina Nunes Silva, Savia Caldeira de Araujo Lopes, Daniel Moreira Santos, Fernanda Silva Torres, Felipe Lima Cardoso, Patricia Massara Martinelli, Elizabeth Ribeiro da Silva, Maria Elena de Lima, Lucas Antonio Ferreira Miranda, Monica Cristina Oliveira
BACKGROUND: PnPP-19 is a 19-amino-acid synthetic peptide previously described as a novel drug for the treatment of erectile dysfunction. OBJECTIVE: The aim of this work was to evaluate the physicochemical properties of cationic transfersomes containing PnPP-19 and the skin permeation of free PnPP-19 and PnPP-19-loaded transfersomes. METHOD: Three different liposomal preparation methods were evaluated. Cationic transfersomes contained egg phosphatidyl choline: stearylamine (9:1 w/w) and Tween 20 (84...
January 8, 2018: Current Drug Delivery
Kamla Pathak, Ankur Vaidya, Vijay Sharma
BACKGROUND: Improvisation of the nanosized vesicular systems has led to a series of useful developments including the deformable vesicles namely transfersomes, ethosomes and invasomes. While the former two have been explored extensively, literature on invasomes is relatively scanty. METHOD: Invasomal formulations researched for various applications have been reviewed using search engine "Scopus". The present review focuses on the update on the research activity on effectiveness and permeation enhancing effects of invasomes for dermal and topical delivery...
January 8, 2018: Current Drug Delivery
R Viswambari Devi, M R Basil-Rose
Lectins are proteins / glycoproteins of non-immunological origin found ubiquitously in all organisms. Research investigations show that many types of diseased tissues often display glycans that vary from their normal counterparts. Therefore, lectins that can interact with these transformed glycans may be used for early diagnosis and treatment of diseases. Specificity of lectins towards glycans has greatly attracted nanobiotechnology in engineering lectin functionalized nanoparticles. Conjugating lectin with a nanosystem can identify and specifically attach to the carbohydrate moieties of glycoproteins expressed on cell surfaces and this has led to the development of several lectin functionalized nanoparticles to target drugs to various tissues with minimized systemic side effects...
January 7, 2018: Current Drug Delivery
Asma Naim, Asma Saeed, Taqdees Ara Malik
In the past few years, the use of antimicrobial drugs against a wide range of pathogens has increased significantly. This extensive use of drugs has increased the resistance rate in microbial community widely. Molecular techniques for the detection of resistance are more reliable as compared to the conventional phenotypic method. The family Enterobacteriaceae is considered to be an important cause of nosocomial infections due to its predominantly active species such as E. coli, Klebsiella and Pseudomonas. These organisms are mainly involved in causing pneumonia, sepsis, post-surgical and urinary tract infections...
January 1, 2018: Current Drug Delivery
Anuja Rode, Sanjay Sharma, Dinesh K Mishra
Nanoscience and nanotechnology are emerging area in pharmaceutical sciences and need of modernizing world. Nanoscience is the world of atoms, macromolecular assemblies, macromolecules, quantum dots, and molecules. Nanoscience is the study, and understanding control of phenomena and manipulation of material at the nanoscale. A carbon nanotubes are tube like the material mainly made up of carbon. Only a carbon nanotubes are the macromolecules of graphite consisting of sheets of carbon, which is weaved into the cylinder...
December 21, 2017: Current Drug Delivery
Shuzhi Qin, Xiangshi Sun, Feng Li, Kongtong Yu, Yulin Zhou, Na Liu, Chengguo Zhao, Lesheng Teng, Youxin Li
Biodegradable nanoparticles with diameters between 100 nm and 500 nm are of great interest in the contexts of targeted delivery. The present work provides a review concerning the effect of binary organic solvents together with emulsifier on particle size as well as the influence of particle size on the in vitro drug release and uptake behavior. The polymeric lipid nanoparticles (PLNs) with different particle sizes were prepared by using binary solvent dispersion method. Various formulation parameters such as binary organic solvent composition and emulsifier types were evaluated on the basis of their effects on particle size and size distribution...
December 21, 2017: Current Drug Delivery
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