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.

scholarly journals Effect of Transcutol and Stearylamine on Ibuprofen Hydrophilic Gel for Transdermal Delivery

2018 ◽  
Vol 8 (01) ◽  
Author(s):  
Mahdi Abd Zair ◽  
D. Prasanthi ◽  
Amoolya Chennuri ◽  
Zainab Rahi Hanthal ◽  
P K Lakshmi
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Skin Irritation ◽  
Oral Drug ◽  
Anti Inflammatory ◽  
Hydrophilic Gel ◽  
Anti Inflammation

Transdermal drug delivery system (TDDS) shows promising results when compared with oral drug delivery system mainly by eliminating the first pass metabolism and by improving the bioavailability of drug. Hydrophilic gels are networks of polymer chains that are sometimes found as colloidal gels in which water is the dispersion medium. Ibuprofen, nonsteroidal anti-inflammatory drug used to relieve pain, reduces fever and anti-inflammation. The purpose of present research is to demonstrate the influence of various enhancers (transcutol and stearylamine) in various concentrations on percutaneous permeation of ibuprofen hydrophilic gel from HPMC K4M & HPMC K100M gel formulation. Gelling agents at various concentrations were preliminary screened for gel consistency. The control and the prepared gels were evaluated for clarity, homogeneity, spreadability, extrudability, drug content, invitro diffusion, ex-vivo permeation, skin irritation, anti-inflammatory activity and stability studies. All formulations have shown better physicochemical properties. Ex-vivo skin permeation studies reveals that the (IBU29) formulated using HPMC K4M 6%, transcutol 40% and stearylamine 4% as permeation enhancers has shown maximum drug release of 86.4 % for 24hrs. Permeability parameters like flux were found to be 1940.68±0.06µg/cm²/hr, permeability coefficient was found 31 ×10-3 cm/hr and Q24 was found to be 5240.82±0.06µg/cm² and enhancement ratio of 13.06 over pure drug. Skin irritation studies showed irritation potential of “0” score thus providing to be non-irritant. The anti-inflammation studies were performed with inflammation induced by carrageenan 1% w/v solution. Optimized formulation (IBU29) showed highest reduction of inflammation comparable to marketed preparation BRUGESIC GEL®. The formulations were stable at room temperature for 1 month.Key words: Transdermal gel, Ibuprofen, HPMC K4M, HPMC K100M, Penetration- enhancer..

scholarly journals Development and Evaluation of Docetaxel-Phospholipid Complex Loaded Self-Microemulsifying Drug Delivery System: Optimization and In Vitro/Ex Vivo Studies

Pharmaceutics ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 544
Author(s):  
Miao Wang ◽  
Sung-Kyun You ◽  
Hong-Ki Lee ◽  
Min-Gu Han ◽  
Hyeon-Min Lee ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Anticancer Agents ◽  
Lipid Membrane ◽  
Ex Vivo ◽  
System Optimization ◽  
Raw Material ◽  
Phospholipid Complex ◽  
Low Solubility

Docetaxel (DTX) has clinical efficacy in the treatment of breast cancer, but it is difficult to develop a product for oral administration, due to low solubility and permeability. This study focused on preparing a self-microemulsifying drug delivery system (SME) loaded with DTX-phospholipid complex (DTX@PLC), to improve the dissolution and gastrointestinal (GI) permeability of DTX. A dual technique combining the phospholipid complexation and SME formulation described as improving upon the disadvantages of DTX has been proposed. We hypothesized that the complexation of DTX with phospholipids can improve the lipophilicity of DTX, thereby increasing the affinity of the drug to the cell lipid membrane, and simultaneously improving permeability through the GI barrier. Meanwhile, DTX@PLC-loaded SME (DTX@PLC-SME) increases the dissolution and surface area of DTX by forming a microemulsion in the intestinal fluid, providing sufficient opportunity for the drug to contact the GI membrane. First, we prepared DTX@PLC-SME by combining dual technologies, which are advantages for oral absorption. Next, we optimized DTX@PLC-SME with nanosized droplets (117.1 nm), low precipitation (8.9%), and high solubility (33.0 mg/g), which formed a homogeneous microemulsion in the aqueous phase. Dissolution and cellular uptake studies demonstrated that DTX@PLC-SME showed 5.6-fold higher dissolution and 2.3-fold higher DTX uptake in Caco-2 cells than raw material. In addition, an ex vivo gut sac study confirmed that DTX@PLC-SME improved GI permeability of DTX by 2.6-fold compared to raw material. These results suggested that DTX@PLC-SME can significantly overcome the disadvantages of anticancer agents, such as low solubility and permeability.

scholarly journals Development of Piperine-Loaded Solid Self-Nanoemulsifying Drug Delivery System: Optimization, In-Vitro, Ex-Vivo, and In-Vivo Evaluation

Nanomaterials ◽  
2021 ◽  
Vol 11 (11) ◽  
pp. 2920
Author(s):  
Ameeduzzafar Zafar ◽  
Syed Sarim Imam ◽  
Nabil K. Alruwaili ◽  
Omar Awad Alsaidan ◽  
Mohammed H. Elkomy ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
Ex Vivo ◽  
In Vitro Release ◽  
System Optimization ◽  
Globule Size

Hypertension is a cardiovascular disease that needs long-term medication. Oral delivery is the most common route for the administration of drugs. The present research is to develop piperine self-nanoemulsifying drug delivery system (PE-SNEDDS) using glyceryl monolinoleate (GML), poloxamer 188, and transcutol HP as oil, surfactant, and co-surfactant, respectively. The formulation was optimized by three-factor, three-level Box-Behnken design. PE-SNEDDs were characterized for globule size, emulsification time, stability, in-vitro release, and ex-vivo intestinal permeation study. The optimized PE-SNEDDS (OF3) showed the globule size of 70.34 ± 3.27 nm, percentage transmittance of 99.02 ± 2.02%, and emulsification time of 53 ± 2 s Finally, the formulation OF3 was transformed into solid PE-SNEDDS (S-PE-SNEDDS) using avicel PH-101 as adsorbent. The reconstituted SOF3 showed a globule size of 73.56 ± 3.54 nm, PDI of 0.35 ± 0.03, and zeta potential of −28.12 ± 2.54 mV. SEM image exhibited the PE-SNEDDS completely adsorbed on avicel. Thermal analysis showed the drug was solubilized in oil, surfactant, and co-surfactant. S-PE-SNEDDS formulation showed a more significant (p < 0.05) release (97.87 ± 4.89% in 1 h) than pure PE (27.87 ± 2.65% in 1 h). It also exhibited better antimicrobial activity against S. aureus and P. aeruginosa and antioxidant activity as compared to PE dispersion. The in vivo activity in rats exhibited better (p < 0.05) antihypertensive activity as well as 4.92-fold higher relative bioavailability than pure PE dispersion. Finally, from the results it can be concluded that S-PE-SNEDDS might be a better approach for the oral delivery to improve the absorption and therapeutic activity.

scholarly journals Genistein Loaded Nanofibers Protect Spinal Cord Tissue Following Experimental Injury in Rats

2018 ◽  
Author(s):  
Mohamed Ismail ◽  
Sara Ibrahim ◽  
Azza Elamir ◽  
Amira M. Elrafei ◽  
Nageh Allam ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Spinal Cord ◽  
Drug Delivery System ◽  
Delivery System ◽  
Enhanced Recovery ◽  
Therapeutic Drug ◽  
Control Group ◽  
Spinal Cord Tissue ◽  
Injured Spinal Cord ◽  
Cord Injury

Implantable drug-delivery systems provide new means for achieving therapeutic drug concentration over a prolonged time to achieve better tissue protection and enhanced recovery. The hypothesis of the current study was to test the antioxidant and anti-inflammatory effects of genistein and nanofibers on the spinal cord tissue following experimental spinal cord injury (SCI). Rats were treated post SCI with genistein loaded on chitosan/polyvinyl alcohol (CS/PVA) nanofibers as an implantable drug-delivery system. SCI caused marked oxidative damage and inflammation as evident by the reduction in the super oxide dismutase (SOD) activity and the level of interleukin-10 (IL-10) in injured spinal cord tissue, as well as, the significant increase in the levels of nitric oxide (NO), malondialdehyde (MDA) and tumor necrosis factor-alpha (TNF-&alpha;). Treatment of rats post SCI with genistein and CS/PVA nanofibers improved most of the above mentioned biochemical parameters and shifted them toward the control group values. Genistein induced an increase in the activity of SOD and the level of IL-10, while causing a decrease in the levels of NO, MDA and TNF-&alpha; in injured spinal cord tissue. Genistein and CS/PVA nanofibers provide a novel combination for treating inflammatory nervous tissue conditions, especially when combined as an implantable drug-delivery system.

A drug delivery system based on switchable photo-controlled p-coumaric acid derivatives anchored on mesoporous silica

2017 ◽  
Vol 5 (4) ◽  
pp. 817-825 ◽  
Author(s):  
Eva Beňová ◽  
Vladimír Zeleňák ◽  
Dáša Halamová ◽  
Miroslav Almáši ◽  
Veronika Petrul'ová ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Mesoporous Silica ◽  
Drug Delivery System ◽  
Delivery System ◽  
Coumaric Acid ◽  
Inflammatory Drug ◽  
Anti Inflammatory

Mesoporous silica modified by p-coumaric acid derivatives as photo-switchable ligands was studied for the delivery of a non-steroidal anti-inflammatory drug.

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