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Current Drug Delivery

Lakshmi Maurya, Sanjay Singh, Mahalingam Rajamanickam Vijayakumar, Hitesh Kumar Dewangan
BACKGROUND: Vinorelbine bitartrate (VRL) is an antimitotic agent approved by FDA for breast cancer and non-small cell lung cancer (NSCLC) in many countries. However, high aqueous solubility and thermo degradable nature of VRL limited the availability of marketed dosage forms. OBJECTIVES: The current work is focused on the development of lipid based aqueous core nanocapsules which can encapsulate the hydrophilic VRL in the aqueous core of nanocapsules protected with a lipidic shell which will further provide a sustained release...
July 15, 2018: Current Drug Delivery
Shindu C Thomas, Tushar Madaan, Zeenat Iqbal, Sushama Talegaonkar
BACKGROUND: Bendamustine HCl, an antineoplastic drug, has a very short life of about 40 minutes which necessitates administration of large doses which leads to increased side effects as well as costs. OBJECTIVE: The present work describes the fabrication, optimization and evaluation of bioactive hydroxyapatite nanoparticles to achieve sustained delivery of bendamustine HCl. METHODS: Hydroxyapatite nanoparticles (NPs) were prepared by the wet chemical precipitation method by reacting a calcium and phosphate precursor and the reaction was optimized via Box-Behnken DOE...
June 20, 2018: Current Drug Delivery
Diana Edwar Aziz, Aly Ahmed Abdelbary, Abdelhalim Ibrahim Elassasy
BACKGROUND: Niosomes are surfactant-based vesicular nanosystems that proved their efficiency in transdermal delivery by overcoming skin inherent anatomic barrier; startum corneum. Central composite design is an efficient tool for developing and optimizing niosomal formulations using fewer experiments. OBJECTIVE: The objective of this study was to prepare niosomes as a transdermal delivery system of diacerein using film hydration technique, employing central composite design, for avoiding its oral gastrointestinal problems...
June 18, 2018: Current Drug Delivery
Lalit Kumar, Shivani Verma, Mehakjot Singh, Tamanna Tamanna, Puneet Utreja
BACKGROUND: Transdermal route of delivery of Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) has several advantages over other routes like reduced adverse effects, less systemic absorption, and avoidance of first pass effect and degradation in the gastrointestinal tract (GIT). Transdermal route is also beneficial for drugs having a narrow therapeutic index. The skin acts as the primary barrier for transdermal delivery of various therapeutic molecules. Various advanced nanocarrier systems offer several advantages like improved dermal penetration along with an extended drug release profile due to their smaller size and high surface area...
June 4, 2018: Current Drug Delivery
Hitesh Kumar Dewangan, Sanjay Singh, Lakshmi Maurya, Amrita Srivastava
The incredibly serious problem of Hepatitis B is virus-related chronic liver disease. The conventional preventive treatment of Hepatitis B requires booster dose, which requires repeated administration of the vaccine to the subject. Thus, there is a need to develop a formulation which can eliminate the need of frequent dosing and enhance patient's acquiescence. To prepare single dose nanovaccine of HBsAg by utilizing central composite design for optimization and interaction of independent variables effects on measured response...
June 3, 2018: Current Drug Delivery
Muhammad Ubaid, Syed Nisar Hussain Shah, Shujaat Ali Khan, Ghulam Murtaza
BACKGROUND: In this study, central composite design was utilized for the optimization of genipin cross-linked chitosan/Eudragit®-L 100 interpenetrating hydrogel network films fabricated through solvent evaporation technique. METHODS: Hydrogel formulations were studied using response surface methodology; regression analysis and the surface plots were used to evaluate the effect of variables on T50% (the time for 50% of drug release) and dynamic swelling with optimum formulation selection...
June 3, 2018: Current Drug Delivery
Yangyang Liu, Beibei Yan, Juan Zhao, Lulu Wang, Yu Gu, Ping Chang, Yancai Wang
The poor penetration and low bioavailability are main challenges for transdermal drug delivery. Nanocrystals technology is an attractive method for water insoluble drug transdermal delivery, as the literature demonstrated that the penetration and bioavailability of the transdermal delivered water insoluble drugs was significantly enhanced and improved by the nanocrystals technology. Currently, the nanocrystals technology has been applied in transdermal delivery of cosmeceutical and for therapy skin diseases, such as diclofenac acid, tretinoin and rutin...
May 18, 2018: Current Drug Delivery
Jaco Heyns, Clarissa Willers, Richard K Haynes, Ho N Wong, Josias H Hamman, Chrisna Gouws
Malaria continues to be a major health concern and affects more than 200 million people a year. Drugs currently used for treatment of malaria are increasingly rendered ineffectual by the ongoing emergence of parasite resistance. For any new drugs, however, knowledge of their membrane permeability is an essential pre-requisite for eventual use. Treatment failure and emergence of resistance can occur as a result of reduced availability of the drug at the desired site of action. Cell-based permeability assays such as Caco-2 cell monolayers serve as a model for predicting drug absorption and efflux, and provide an estimate of drug bioavailability...
May 18, 2018: Current Drug Delivery
Elisabetta Esposito, Alessandra Pecorelli, Maddalena Sguizzato, Markus Drechsler, Paolo Mariani, Federica Carducci, Franco Cervellati, Rita Cortesi, Giuseppe Valacchi
BACKGROUND: Wound healing is a biological process that can get in a state of pathologic inflammation, requiring the use of specific medications able to promote proper tissue repair. OBJECTIVE: The study describes the production and characterization of nanoparticle based gel for wound healing treatment designed to deliver hyaluronic acid and retinyl palmitate onto the skin. METHOD: Tristearin solid lipid nanoparticles and nanostructured lipid carriers based on a tristearin and caprylic/capric triglyceride mixture were produced and characterized...
May 18, 2018: Current Drug Delivery
Romeo Ngoune, Christine Contini, Michael Marcus Hoffmann, Dominik Elverfeldt, Karl Winkler, Gerhard Putz
BACKGROUND: Nanoscale drug delivery systems accumulate in solid tumors preferentially by the enhanced permeation and retention effect (EPR-effect). Nevertheless, only a miniscule fraction of a given dosage reaches the tumor, while >90% of the given drug ends up in otherwise healthy tissues, leading to the severe toxic reactions observed during chemotherapy. Once accumulation in tumor has reached its maximum, extracorporeal elimination of circulating nanoparticles by plasmapheresis can diminish toxicities...
May 18, 2018: Current Drug Delivery
Jose Luis Pedraz, Manoli Igartua, Rosa Maria, Sara Hernando
Nanomedicine is a field of science that employs materials in the nanometer scale. Specifically, the use of nanoparticles (NPs) has some medical applications due to their structure, for example, the ability to cross the biological barriers, and their effectiveness avoiding some drug delivery problems. Because of that, in the last years, the use of NPs has been raised as a workable solution for neurodegenerative diseases (ND) treatment [1,2]. NDs are characterized by a continuous structural and functional neuronal loss, usually correlated with neuronal death...
May 9, 2018: Current Drug Delivery
Giovanni Monastra, Simonetta Ferruzza, Yula Sambuy, Giulia Ranaldi, Daniela Ferrari
BACKGROUND: . Myo-inositol is a natural molecule with important therapeutic applications and an impaired oral absorption may result in a reduced clinical effect. Aim of this study was to determine if the combined oral administration of α-lactalbumin and myo-inositol in healthy subjects, could increase the plasma level of myo-inositol administered alone. In vitro studies on human differentiated intestinal Caco-2 cells were also conducted to identify the mechanisms involved in myo-inositol absorption...
May 8, 2018: Current Drug Delivery
Himanshu Bhatt, Sri Vishnu Kiran Rompicharla, Neeraja Komanduri, Aashma Shah, Sateja Paradkar, Balaram Ghosh, Swati Biswas
BACKGROUND: Solid lipid nanoparticles (SLNs) represent an affordable, easily scalable, stable and biocompatible drug delivery system with a high drug to lipid ratio which also improves solubility of poorly soluble drugs. OBJECTIVE: SLNs were developed by using glyceryl monostearate as the single lipid in presence of surfactant Poloxamer 188 and evaluated the efficiency of the SLNs to load the therapeutic cargo, curcumin (CUR). METHOD: The nano-formulation was optimized by Quality by Design approach to understand the effect of various process parameters on various quality attributes, including drug loadability, particle size and polydispersity...
May 3, 2018: Current Drug Delivery
Marcela Brito Oliveira, Jessica Bassi da Silva, Maiara Camotti Montanha, Elza Kimura, Andrea Diniz, Marcos Luciano Bruschi
BACKGROUND: Bladder cancer is the second type of malignant carcinoma of the urinary tract. The treatment is time-consuming and requires maintenance doses of the drug for long periods of time with important side effects. Curcumin has shown evident clinical advances in the treatment of cancer. The technology of microencapsulation and the use of mucoadhesive materials can contribute to modify the delivery and improve the bioavailability of curcumin. OBJECTIVE: The aim of this study was to design and characterize mucoadhesive microparticles containing curcumin using multivariate analysis and the spray-drying technique...
May 3, 2018: Current Drug Delivery
Subhasis Chakrabarty, Bijaya Ghosh, Tapan Kumar Giri, Jasmina Khanam
The work was aimed at extracting gabapentin by transdermal reverse iontophoresis to check its feasibility for noninvasive therapeutic drug monitoring. Gabapentin was delivered in phosphate buffer (pH 7.4) at a therapeutic concentration range of 2-10 µg/ml. The same media was also used in receiver compartment. Extractions were carried out under an electric field of 5 V (current intensity range 0.3 mA/cm2-0.5 mA/cm2), provided by a custom-made power source for a period of 4 h. Samples were withdrawn at hourly intervals and drug content was analyzed by HPLC...
May 3, 2018: Current Drug Delivery
Vasanthan Ravichandran, Venkitasamy Kesavan, Sandrine Cojean, Philippe M Loiseau, Athipettah Jayakrishnan
BACKGROUND: Amphotericin B (AmB), a polyene antibiotic used for the treatment of fungal and leishmanial infections is virtually insoluble in water and exhibits severe toxicity. AmB has been conjugated to various soluble polymers for improving its solubility and reducing its toxicity. Conjugating AmB to a polysorbate surfactant such as polyoxyethylene sorbitan monolaurate (Tween 20), was examined to improve its solubility and reduce its toxicity. METHODS: AmB was coupled to Tween 20 via carbamate linkage at 15 and 30 wt% concentrations in high yield by activating the hydroxyl groups of the surfactant using p- nitrophenyl chloroformate...
May 3, 2018: Current Drug Delivery
Muhammad Zia Ullah Khan, Petre Makreski, Ghulam Murtaza
The aim of present explorative study was to prepare and optimize finasteride loaded topical gel formulations by using three factor [propylene glycol (PG), Tween® 80, and sodium lauryl sulphate (SLS)], five level central composite design. Optimized finasteride topical gel formulation (F4), containing PG, Tween® 80, and SLS in a concentration of 0.8 mg, 0.4 mg and 0.2 mg, respectively, showed 6-fold higher values of cumulative drug release, flux, partition coefficient, input rate, lag time, and diffusion coefficient, when compared to control formulation without permeation enhancer...
May 2, 2018: Current Drug Delivery
Lakshmi Maurya, Vijayakumar Mahalingam Rajamanickam, Gopeshwar Narayan, Sanjay Singh
BACKGROUND: Vinorelbine bitartrate (VRL), a semi synthetic vinca alkaloid approved for breast cancer, has been proved to beneficial as first line and subsequent therapies. However, it's hydrophilic and thermo labile nature provides hindrance to oral clinical translation. OBJECTIVES: The current work focused on the application of DOE a modern statistical optimization tool for the development and optimization of a solid lipid nanoparticle (SLN) formulation that can encapsulate hydrophilic and thermolabile Vinorelbine bitartrate (VRL) to a maximum extent without compromising integrity and anticancer activity of the drug...
April 8, 2018: Current Drug Delivery
Ligia Santos Pedroso, Najeh Maissar Khalil, Rubiana Mara Mainardes
In this study, bovine serum albumin (BSA) nanoparticles coated with polysorbate-80 (PS-80) and containing amphotericin B (AmB) were developed using a coacervation method. The nanoparticles were spherical, had a uniform size distribution (polydispersity < 0.25), a small mean size (185 ± 5 nm), a high zeta potential (-38.0 ± 0.7 mV), and a high AmB encapsulation efficiency (93 ± 1%). The AmB release profile was prolonged and diffusion-controlled, resulting in a low degree of AmB aggregation in solution...
April 8, 2018: Current Drug Delivery
Muhammad Ubaid, Ghulam Murtaza
In this study, central composite factorial design was used for the preparation and optimization of chitosan/Na-alginate hydrogel films containing metformin via solvent evaporation technique. Low and high molecular weight (MW) chitosan was used as polymer in different concentrations while genipin was used as crosslinking agent. Drug release studies were performed in simulated gastric and intestinal fluids at pH 1.2 and 7.4 of formulated hydrogels. For low MW chitosan hydrogel, the highest drug release at pH 1...
April 8, 2018: Current Drug Delivery
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