scholarly journals Combinatorial therapeutic drug delivery of riboflavin and dexamethasone for the treatment of keratoconus affected corneas of mice: Ex vivo permeation and hemolytic toxicity

2021 ◽  
Author(s):  
Na Wo ◽  
Jiabin Zhai
Keyword(s):  
Drug Delivery ◽  
Ex Vivo ◽  
Therapeutic Drug ◽  
Ex Vivo Permeation ◽  
Hemolytic Toxicity

Nanostructured Lipid Carriers for Intranasal Administration of Olanzapine in the management of Schizophrenia

2021 ◽  
Vol 14 ◽  
Author(s):  
Sarbjot Kaur ◽  
Ujjwal Nautiyal ◽  
Pooja A. Chawla ◽  
Viney Chawla
Keyword(s):  
Drug Delivery ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Nanostructured Lipid Carriers ◽  
Polydispersity Index ◽  
Poloxamer 407 ◽  
Ex Vivo Permeation ◽  
Permeation Studies ◽  
Vitro Release

Background: Background: Olanzapine belongs to a new class of dual spectrum antipsychotic agents. It is known to show promise in managing both the positive and negative symptoms of schizophrenia. Drug delivery systems based on nanostructured lipid carriers (NLC) are expected to provide rapid nose-to-brain transport of this drug and improved distribution into and within the brain. Objective: The present study deals with the preparation and evaluation of olanzapine loaded NLC via the intranasal route for schizophrenia. Methods: Olanzapine-NLC were formulated through the solvent injection method using isopropyl alcohol as the solvent, stearic acid as solid lipid, and oleic acid as liquid lipid, chitosan as a coating agent, and Poloxamer 407 as a surfactant. NLC were characterized for particle size, polydispersity index, entrapment efficiency, pH, viscosity, X-ray diffraction studies, in-vitro mucoadhesion study, in- vitro release and ex-vivo permeation studies. The shape and surface morphology of the prepared NLC was determined through transmission electron microscopy. To detect the interaction of the drug with carriers, compatibility studies were also carried out. Results: Average size and polydispersity index of developed formulation S6 was 227.0±6.3 nm and 0.460 respectively. The encapsulation efficiency of formulation S6 was found to be 87.25 %. The pH, viscosity, in-vitro mucoadhesion study, and in- vitro release of optimized olanzapine loaded NLC were recorded as 5.7 ± 0.05, 78 centipoise, 15±2 min, and 91.96 % respectively. In ex-vivo permeation studies, the percent drug permeated after 210 min was found to be 84.03%. Conclusion: These results reveal potential application of novel olanzapine-NLC in intranasal drug delivery system for treatment of schizophrenia.

scholarly journals SCIDOT-18. NANOTHERAPEUTICS FOR NEUROSURGICALLY-APPLIED DRUG DELIVERY

2019 ◽  
Vol 21 (Supplement_6) ◽  
pp. vi275-vi275
Author(s):  
Catherine Vasey ◽  
Vincenzo Taresco ◽  
Stuart Smith ◽  
Cameron Alexander ◽  
Ruman Rahman
Keyword(s):  
Drug Delivery ◽  
Ex Vivo ◽  
Drug Formulation ◽  
Local Drug Delivery ◽  
Resection Margins ◽  
Therapeutic Drug ◽  
Tumour Resection ◽  
Combination Drug ◽  
Drug Encapsulation ◽  
Drug Concentrations

Abstract Design and implementation of innovative local drug delivery systems (DDS) may overcome current limitations in GBM treatment, such as the lack of therapeutic drug concentrations reaching residual GBM cells following surgery. Here we describe a novel DDS which utilises a bespoke mechanically engineered spray device, designed for safe surgical use, to deliver a mucoadhesive hydrogel containing chemotherapeutic nanoparticles (NPs) into the tumour resection margins. The overall aim is to spray a NP and polymer solution onto the resection cavity and potentially increase penetration of anti-cancer drugs within the 2 cm reoccurrence zone beyond the infiltrative margin. The mucoadhesive gel of choice, pectin, is currently used in other in vivo applications; however we have repurposed this for the brain. Pectin is biocompatible with GBM and human astrocyte cells in vitro and showed neither toxicity nor inflammation for up to 2 weeks upon orthotopic brain injection. Pectin is biodegradable in artificial CSF and is capable of being sprayed from the engineered device. A panel of polymeric, oil-based and polymer-coated NPs have been developed and optimised to maximise drug encapsulation of etoposide and olaparib as proof-of-concept for combination drug delivery. Etoposide/olaparib was chosen due to cytotoxicity from 5 GBM cell lines, including primary lines isolated from the invasive tumour margin (Mean IC50 of 1.1 µM and 8.3 µM respectively). The optimal NP/drug formulation (based on drug encapsulation, spray capability and bio-adhesiveness) will ultimately be assessed for tolerability and efficacy using orthotopic allograft and xenograft high-grade glioma models, including measurement of penetration of drug/nanoparticle in ex vivo murine and porcine brain using novel hybrid time-of-flight/Orbitrap TM secondary ion mass spectrometer (orbiSIMS) technology.

Imidazolium-Based Ionic Liquid-Assisted Preparation of Nano-Spheres Loaded with Bio-Active Peptides to Decrease Inflammation in an Osteoarthritis Model: Ex Vivo Evaluations

2021 ◽  
Vol 17 (5) ◽  
pp. 859-872
Author(s):  
Yingzhuo Song ◽  
Tao Zhang ◽  
Huiguang Cheng ◽  
Wei Jiang ◽  
Pu Li ◽  
...  
Keyword(s):  
Electron Microscopy ◽  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ex Vivo ◽  
Cartilage Explants ◽  
Therapeutic Drug ◽  
Therapeutic Peptides ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

Osteoarthritis is one of the most prevalent chronic diseases. Cartilage inflammation in osteoarthritis results from pain in articular joints. Anti-inflammatory drugs provide relief by hindering the production of pro-inflammatory cytokines and interleukin-6. Targeted delivery of anti-inflammatory drugs is very effective in the treatment of osteoarthritis. This approach reduces the usage of therapeutic drug dosages and unwanted side effects. Here, we fabricated a non-invasive and efficient targeted drug delivery system to reduce persistent inflammation in an osteoarthritis model. Temperature-sensitive hollow dextran/poly(N-isopropyl acrylamide) nanoparticles were synthesized by the destruction of N,N’-bis(acryloyl)cystamine crosslinked cores in imidazolium-based ionic liquids. The copolymerized 2-acrylamido-2-methylpropane sulfonic acid created sulfur functionalities that increase the loading of therapeutic KAFAK peptides. The chemical structure of the polymer nanoparticles was analyzed with UV-Visible, Fourier transform infrared, and X-ray photoelectron spectroscopy. The thermal responsive characteristics of the nanoparticles were determined with dynamic light scattering, scanning electron microscopy, and transmission electron microscopy analyses. Moreover, the synthesized nanoparticles were used as drug carriers to reduce inflammation in an Ex Vivo osteoarthritis model. The KAFAK-loaded hollow dextran/PNIPAM nanoparticles effectively delivered therapeutic peptides in cartilage explants to suppress inflammation. These thermoresponsive nanoparticles could be an effective drug delivery system to deliver anti-inflammatory therapeutic peptides in a highly osteoarthritic environment.

Combinatorial Therapeutic Drug Delivery of Riboflavin and Olopetadine for the Treatment of Keratoconus Affected Corneas of Mice

2019 ◽  
Vol 9 (5) ◽  
pp. 668-672
Author(s):  
Geqiang Yang ◽  
Yushun Xue ◽  
Yanni Zhu ◽  
Ying Qin ◽  
Jing Zhang
Keyword(s):  
Drug Delivery ◽  
Ex Vivo ◽  
Methyl Cellulose ◽  
Therapeutic Drug ◽  
The Novel ◽  
Mice Model ◽  
Gelation Temperature ◽  
Gelling Temperature ◽  
Thermoreversible Gel ◽  
Evaluation Parameters

The present study deals with the development and evaluation of novel thermoreversible gel containing Riboflavin and Olopatadine for the treatment of Keratoconus. The novel gel was prepared by using polymers like Poloxamer and hydroxypropyl methyl cellulose (HPMC) using cold method. The formulated system was evaluated for clarity, appearance, pH, gelling temperature, ex vivo diffusion study, Isotonicity, hemolytic study and effect in keratoconus affected mice model. The results showed that formulated gel was found to be clear and transparent having high gelling capacity. The pH was found between 6.5 to 6.9 and gelation temperature between 34 to 37 °C. All formulations were found isotonic and the hemolytic study performed proved the non-hemolytic nature of formulation. Drug content was also within acceptable limit. The F5 formulation was found to be optimized considering all evaluation parameters. F5 formulation showed maximum amount of release (98.5 and 99.6% for Ribo and Olo respectively) within 8 hrs as compare to other formulations. The effect of formulation on keratoconus affected mice showed that matrix can be produced after stimulation of KC cells and the increased thickness can be result of increase number of cells or matrix produced per cell. These results clearly conclude the potential of combinatorial therapeutic drug delivery of riboflavin and olopetadine for the treatment of keratoconus affected corneas of mice.

scholarly journals EFFECT OF POLYMERIC BLEND ON EX-VIVO PERMEATION STUDIES OF ACECLOFENAC LOADED FILM FORMING GEL

2021 ◽  
pp. 117-122
Author(s):  
HIMANI BAJAJ ◽  
VINOD SINGH ◽  
RANJIT SINGH ◽  
TIRATH KUMAR
Keyword(s):  
Drug Delivery ◽  
Transdermal Drug Delivery ◽  
Ex Vivo ◽  
Prepared Film ◽  
Variable Effect ◽  
Ex Vivo Permeation ◽  
Film Forming ◽  
Transdermal Drug Delivery Systems ◽  
Permeation Studies ◽  
Polymeric Blend

Objective: To date, film-forming systems have been intensively investigated for transdermal drug delivery. Film-forming systems offers various advantages compared over conventional transdermal drug delivery systems. The objective of the present study was to study the effect of polymeric blend on ex-vivo permeation studies of topical film-forming gel of aceclofenac. Methods: Film-forming gels were prepared by using Hydroxypropyl methylcellulose and Eudragit polymeric blend in varied concentrations, polyethylene glycol 400 as plasticizer, ethanol as solvent and tween 80 as a penetration enhancer. The prepared film-forming gels were evaluated and the influence of the concentration and ratio of polymeric blends used plasticizer and ethanol were investigated. Results: All the prepared film-forming gels showed satisfactory properties regarding homogeneity, compatibility, viscosity and pH value. Variation in the concentration of polymers showed a variable effect on drug permeation rate from film-forming gels. Almost, all formulations permeated up to 80% of drug in 12 h and formulation F1 showed a maximum release about 97.54 % in 12 h. Conclusion: Film-forming gels of aceclofenac with sustained-release profile were successfully developed and may provide a promising effective formulation which may improve patient compliance.

Optimization and Evaluation of Self-nanoemulsifying Drug Delivery System for Enhanced Bioavailability of Plumbagin

Planta Medica ◽  
2021 ◽  
Author(s):  
Pavan Ram Kamble ◽  
Karimunnisa Sameer Shaikh
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Bioavailability ◽  
Ex Vivo ◽  
The Self ◽  
Equilibrium Solubility ◽  
Ex Vivo Permeation ◽  
Ex Vivo Permeation Study

AbstractPlumbagin, a potential bioactive lipophilic molecule, possesses limited solubility and low oral bioavailability. The purpose of the present study was to examine the potential of the self-nanoemulsifying drug delivery system for improving solubility and oral bioavailability of plumbagin. The self-nanoemulsifying drug delivery system was formulated from Capmul MCM (oil), Tween 20 (surfactant), and propylene glycol (cosurfactant). Central composite design was employed as statistical tool to optimize the formulation variables, X1 (oil) and X2 (surfactant: co-surfactant mixture ratio), of the self-nanoemulsifying drug delivery system. The responses studied were droplet size, self-emulsification time, % of drug release in 15 min, and equilibrium solubility. The optimized liquid self-nanoemulsifying drug delivery system was adsorbed on Neusilin US2 and characterized for flow properties, X-ray diffractometry, differential scanning calorimetry, in vitro dissolution, in vivo anti-inflammatory activity, and bioavailability study in Wistar rats, as well as ex vivo permeation study. The droplet size, polydispersity index, self-emulsification time, and equilibrium solubility of the optimized formulation were 58.500 ± 1.170 nm, 0.228 ± 0.012, 17.660 ± 1.520 s, and 34.180 ± 1.380 mg/mL, respectively. Its zeta potential, transmittance value, and cloud point were − 28.200 ± 1.200 mV, 99.200% ± 0.600, and 90 °C, respectively. Drug release was found to be 93.320% ± 1.090. In vivo anti-inflammatory study confirmed more enhanced activity from the self-nanoemulsifying drug delivery system than with pure plumbagin. Pharmacokinetic study in rats revealed that solid self-nanoemulsifying drug delivery system had 4.49-fold higher bioavailability than pure plumbagin. Ex vivo permeation study demonstrated 1.75-fold increased intestinal permeability of the self-nanoemulsifying drug delivery system than pure plumbagin. The developed self-nanoemulsifying drug delivery system is a useful solid platform for improving solubility and oral bioavailability of plumbagin.

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