scholarly journals Formulation and Optimization of Polymeric Nanoparticles for Intranasal Delivery of Lorazepam Using Box-Behnken Design:In VitroandIn VivoEvaluation

2014 ◽  
Vol 2014 ◽  
pp. 1-14 ◽  
Author(s):  
Deepak Sharma ◽  
Dipika Maheshwari ◽  
Gilphy Philip ◽  
Ravish Rana ◽  
Shanu Bhatia ◽  
...  
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Cell Viability ◽  
Ex Vivo ◽  
Burst Release ◽  
Release Behavior ◽  
Sprague Dawley ◽  
Drug Release Behavior ◽  
Biodistribution Studies

The aim of the present study was to optimize lorazepam loaded PLGA nanoparticles (Lzp-PLGA-NPs) by investigating the effect of process variables on the response using Box-Behnken design. Effect of four independent factors, that is, polymer, surfactant, drug, and aqueous/organic ratio, was studied on two dependent responses, that is,z-average and % drug entrapment. Lzp-PLGA-NPs were successfully developed by nanoprecipitation method using PLGA as polymer, poloxamer as surfactant and acetone as organic phase. NPs were characterized for particle size, zeta potential, % drug entrapment, drug release behavior, TEM, and cell viability. Lzp-PLGA-NPs were characterized for drug polymer interaction using FTIR. The developed NPs showed nearly spherical shape withz-average 167–318 d·nm, PDI below 0.441, and −18.4 mV zeta potential with maximum % drug entrapment of 90.1%.In vitrodrug release behavior followed Korsmeyer-Peppas model and showed initial burst release of21.7±1.3%with prolonged drug release of69.5±0.8%from optimized NPs up to 24 h.In vitrodrug release data was found in agreement withex vivopermeation data through sheep nasal mucosa.In vitrocell viability study on Vero cell line confirmed the safety of optimized NPs. Optimized Lzp-PLGA-NPs were radiolabelled with Technitium-99m for scintigraphy imaging and biodistribution studies in Sprague-Dawley rats to establish nose-to-brain pathway.

scholarly journals Nanoformulation and Evaluation of Oral Berberine-Loaded Liposomes

Molecules ◽  
2021 ◽  
Vol 26 (9) ◽  
pp. 2591
Author(s):  
Thuan Thi Duong ◽  
Antti Isomäki ◽  
Urve Paaver ◽  
Ivo Laidmäe ◽  
Arvo Tõnisoo ◽  
...  
Keyword(s):  
Thin Film ◽  
Drug Release ◽  
Size Distribution ◽  
Water Soluble ◽  
Release Behavior ◽  
Uniform Size ◽  
Ethanol Injection ◽  
Drug Release Behavior ◽  
Poorly Water Soluble

Berberine (BBR) is a poorly water-soluble quaternary isoquinoline alkaloid of plant origin with potential uses in the drug therapy of hypercholesterolemia. To tackle the limitations associated with the oral therapeutic use of BBR (such as a first-pass metabolism and poor absorption), BBR-loaded liposomes were fabricated by ethanol-injection and thin-film hydration methods. The size and size distribution, polydispersity index (PDI), solid-state properties, entrapment efficiency (EE) and in vitro drug release of liposomes were investigated. The BBR-loaded liposomes prepared by ethanol-injection and thin-film hydration methods presented an average liposome size ranging from 50 nm to 244 nm and from 111 nm to 449 nm, respectively. The PDI values for the liposomes were less than 0.3, suggesting a narrow size distribution. The EE of liposomes ranged from 56% to 92%. Poorly water-soluble BBR was found to accumulate in the bi-layered phospholipid membrane of the liposomes prepared by the thin-film hydration method. The BBR-loaded liposomes generated by both nanofabrication methods presented extended drug release behavior in vitro. In conclusion, both ethanol-injection and thin-film hydration nanofabrication methods are feasible for generating BBR-loaded oral liposomes with a uniform size, high EE and modified drug release behavior in vitro.

Nano-Surface Modification on Titanium Implants for Drug Delivery

2007 ◽  
Vol 1054 ◽  
Author(s):  
Chang Yao ◽  
Thomas J Webster
Keyword(s):  
Drug Release ◽  
Surface Engineering ◽  
Physical Adsorption ◽  
Titanium Implants ◽  
Orthopedic Implant ◽  
Release Behavior ◽  
Oh Groups ◽  
Chemically Modified ◽  
Drug Release Behavior

ABSTRACTThe surface layer of titanium implants, i.e. titanium dioxide, is responsible for the inertness of titanium-based implants within the human body. However, their cytocompatibility properties and long-term efficacy are limited without further surface engineering since the average functional lifetime of an orthopedic implant is only 10 to 15 years. In this study, an electrochemical method known as anodization was used to create titania nanotubular structures on titanium implant surfaces. These nanotubes were about 60 nm wide (inner diameter) and 200 nm deep. In vitro studies found that anodized surfaces consisting of titania nanotube arrays were favored by bone-forming cells (osteoblasts) compared to unanodized surfaces. These titania nano-tubular structures were utilized here as novel drug release delivery systems. It is proposed that the system designed here can have multi-functional drug release to inhibit infection and wound inflammation while increasing new bone formation. For this purpose, antibiotic drugs (penicillin and streptomycin) were loaded into these nanotubular structures by physical adsorption. To mediate interactions between drug molecules and nanotube walls, anodized titanium nanotubes were modified by silanization to possess amine or methyl groups on their surface instead of −OH groups. Results showed increased hydrophobicity of chemically modified titania nanotubes (methyl > amine > hydroxyl terminated surface). These drug loaded substrates were soaked in phosphate buffered solution in a simulated body environment to determine drug release behavior. Buffer solutions were collected and replaced every day. The eluted drug amounts were measured spectroscopically. Results showed more antibiotic penicillin and streptomycin released from chemically modified nanotubes compared to unanodized titanium substrates; specifically, titania anodized nanotubes functionalized with −OH groups did quite well. In this manner, this study advances titanium currently used in orthopedics to possess drug release behavior which can improve orthopedic implant efficacy.

scholarly journals FORMULATION AND CHARACTERIZATION OF PAPAIN LOADED SOLID LIPID NANOPARTICLES AGAINST HUMAN COLORECTAL ADENOCARCINOMA CELL LINE

2018 ◽  
Vol 11 (10) ◽  
pp. 393
Author(s):  
Suriyakala Perumal Chandran ◽  
Kannikaparameswari Nachimuthu
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Cell Viability ◽  
Cell Line ◽  
Solid Lipid Nanoparticles ◽  
Colorectal Adenocarcinoma ◽  
Lipid Nanoparticles ◽  
In Vitro Drug Release

Objective: Colorectal cancer is one of the most commonly diagnosed cancer and also most common gastrointestinal malignancy with high prevalence rate in the younger population. Usually, cancer cells are surrounded by a fibrin coat which is resistant to fibrinolytic degradation. This fibrin coat is act as self-protective against natural killing mechanism. The main objective was to prepare papain-loaded solid lipid nanoparticles (P-SLN) by melt dispersion-ultrasonication method and investigated the cytotoxic efficacy against colorectal adenocarcinoma (human colorectal adenocarcinoma [HCT 15]) cells.Methods: Optimized polymer ratio was characterized by differential scanning calorimetry, Fourier-transform infrared, X-ray diffraction, scanning electron microscopy, entrapment efficiency, particle size and zeta potential analysis, in vitro drug release, and in vitro cytotoxicity studies on HCT-15 colorectal adenocarcinoma cells.Results: The results showed that the particle size, morphological character and zeta potential value of optimized batch P-SLN were 265 nm, spherical and −26.5 Mv, respectively. The in vitro drug profile of P-SLN exhibited that it produced sustain drug release, and the cell viability of HCT-15 against P-SLN shown better efficacy than pure papain enzyme.Conclusion: P-SLNs were successfully prepared and investigated the in vitro drug release and in vitro cell viability against HCT-15 cell line.

scholarly journals Preparation and Characterization of Coaxial Electrospinning rhBMP2-Loaded Nanofiber Membranes

2019 ◽  
Vol 2019 ◽  
pp. 1-13 ◽  
Author(s):  
He Zhao ◽  
Yali Ma ◽  
Dahui Sun ◽  
Wendi Ma ◽  
Jihang Yao ◽  
...  
Keyword(s):  
Cell Proliferation ◽  
Drug Release ◽  
Osteogenic Differentiation ◽  
Release Behavior ◽  
Promote Cell Proliferation ◽  
Drug Release Behavior ◽  
One Step ◽  
Nanofiber Membranes ◽  
Dual Release

DEX and rhBMP2-loaded core-shell nanofiber membranes were synthesized by electrospinning method in one step. Zein/PLLA, Zein-DEX/PLLA, Zein/PLLA-rhBMP2, and Zein-DEX/PLLA-rhBMP2 were fabricated; and morphology, hydrophilicity, mechanics properties, in vitro drug release behavior, cell proliferation, and osteogenic differentiation were investigated. The results showed that the dual-release system containing rhBMP2 and DEX prepared by electrospinning had rough surface, constant drug release behavior, and could also significantly promote cell proliferation and osteogenic differentiation of RMSCs, indicating that the scaffolds we fabricated might be suitable for bone tissue engineering.

scholarly journals FORMULATION OF POLYMERIC NANOSUSPENSION CONTAINING PRAMIPEXOLE DIHYDROCHLORIDE AND HESPERIDIN FOR IMPROVED TREATMENT OF PARKINSON’S DISEASES

2018 ◽  
Vol 11 ◽  
Author(s):  
Somasundaram I
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Burst Release ◽  
Drug Content ◽  
Pramipexole Dihydrochloride ◽  
Vitro Release

Aims and Objectives: The present study is to formulate the nanosuspension containing a hydrophilic drug pramipexole dihydrochloride and hesperidin and to increase the drug entrapment efficiency.Methods: Hesperidin and pramipexole dihydrochloride loaded in chitosan nanosuspension is prepared by ionic gelation method using chitosan and tripolyphosphate. There was no incompatibility observed between the drug and polymer through Fourier transform infrared and differential scanning calorimetric. Various other parameters such as particle size, zeta potential, scanning electron microscope, drug content, drug entrapment efficiency, and in vitro release have been utilized for the characterization of nanoparticles.Results and Discussion: The average size of particle is 188 nm; zeta potential is 46.7 mV; drug content of 0.364±0.25 mg/ml; entrapment efficiency of 72.8% is obtained with HPN3 formulation. The PHC1 shows the highest drug release followed by PHC2 due to low concentration of polymer and PHC4 and PHC5 show less drug release due to high concentration of polymer. The in vitro release of PHC3 is 85.2%, initial the burst release is shown which is approximately 60% in 8 h; then, slow release later on drastic reduction in release rate is shown in 24 h. The in vivo study histopathological report confers the effective protective against rotenone induces Parkinson’s.Conclusion: PHC3 was chosen as the best formulation due to its reduced particle size and controlled release at optimum polymer concentration which may be used to treat Parkinson’s disease effectively..

Sustained drug release using cobalt oxide nanowires for the preparation of polymer-free drug-eluting stents

2018 ◽  
Vol 33 (3) ◽  
pp. 352-362 ◽  
Author(s):  
Tarek M Bedair ◽  
Il Jae Min ◽  
Wooram Park ◽  
Yoon Ki Joung ◽  
Dong Keun Han
Keyword(s):  
Drug Release ◽  
Cobalt Oxide ◽  
Drug Eluting Stents ◽  
Therapeutic Drug ◽  
Burst Release ◽  
Release Behavior ◽  
Cobalt Chromium ◽  
Oxide Nanowires ◽  
Drug Eluting

Polymer-based drug-eluting stents (DESs) represented attractive application for the treatment of cardiovascular diseases; however, polymer coating has caused serious adverse responses to tissues such as chronic inflammation due to acidic by-products. Therefore, polymer-free DESs have recently emerged as promising candidates for the treatment; however, burst release of drug(s) from the surface limited its applications. In this study, we focused on delivery of therapeutic drug from polymer-free (or -less) DESs through surface modification using cobalt oxide nanowires (Co3O4 NWs) to improve and control the drug release. The results demonstrated that Co3O4 NWs could be simply fabricated on cobalt–chromium substrate by ammonia-evaporation-induced method. The Co3O4 NWs were uniformly arrayed with diameters of 50–100 nm and lengths of 10 µm. It was found that Co3O4 NWs were comparatively stable without any delamination or change of the morphology under in vitro long-term stability using circulating system. Sirolimus was used as a model drug for studying in vitro release behavior under physiological conditions. The sirolimus release behavior from flat cobalt–chromium showed an initial burst (over 90%) after one day. On the other hand, Co3O4 NWs presented a sustained sirolimus release rate for up to seven days. Similarly, the polymer-less specimens on Co3O4 NWs substrates sustained sirolimus release for a longer-period of time when compared to flat Co–Cr substrates. In summary, the current approach of using Co3O4 NWs-based substrates might have a great potential to sustain drug release for drug-eluting implants and medical devices including stents.

Plasmonic CuS nanodisk assembly based composite nanocapsules for NIR-laser-driven synergistic chemo-photothermal cancer therapy

2018 ◽  
Vol 6 (7) ◽  
pp. 1035-1043 ◽  
Author(s):  
Jian He ◽  
Lisha Ai ◽  
Xin Liu ◽  
Hao Huang ◽  
Yuebin Li ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Drug Release ◽  
Cancer Cells ◽  
Therapeutic Effects ◽  
Release Behavior ◽  
Sustained Drug Release ◽  
Drug Release Behavior ◽  
Nir Laser

The NIR-laser-driven plasmonic photothermal and sustained drug release behavior of CuS–PTX/SiO2 nanocapsules show great synergistic chemo-photothermal therapeutic effects on cancer cells in vitro and in vivo.

scholarly journals Development and Optimization of Proniosomal Gel Containing Etodolac: In-vitro, Ex-vivo and In-vivo Evaluation

2021 ◽  
Vol 62 (3) ◽  
pp. 290-304
Author(s):  
Moreshwar Patil ◽  
Prashant Pandit ◽  
Pavan Udavant ◽  
Sandeep Sonawane ◽  
Deepak Bhambere
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
In Vivo Evaluation ◽  
Vesicle Size ◽  
Skin Delivery ◽  
The Stability

Introduction: Etodolac is used in the treatment of acute pain and inflammation. It has low solubility because of high hydrophobicity and it is reported that upon oral administration shows gastric disturbances. This encourages the development of topical vesicular formulation. Method: In this work we used coacervation-phase separation method for the development of etodolac loaded vesicular system by using non-ionic surfactants, cholesterol and soya lecithin. Central composite design (rotatble) was used to optimize the concentrations of soy lecithin, surfactant and cholesterol. The prepared formulations were characterized by number of vesicles formed, vesicle size, zeta potential, entrapment efficiency, in-vitro permeation, ex-vivo permeation and anti-inflammatory study. Results: Etodolac was successfully entrapped in all formulations having efficiency in the range of 74.36% to 90.85%, which was more at 4 °C than room temperature. When hydrated with water; niosome in the range of 54 to 141 (per cubic mm) were spontaneously produced. The results of in-vitro diffusion study revealed that etodolac was released in the range of 71.86 to 97.16% over a period of 24 hrs. The average vesicle size of optimized formulation was found 211.9 nm with PDI of 0.5. The observed responses i.e. % encapsulation efficiency and drug release were 74.12 and 95.08 respectively. The zeta potential was -19.4mV revealed the stability of formulation which was further confirmed by no changes in drug content and drug release after stability studies. The % inhibition in paw volume was 40.52% and 43.61% for test and marketed proniosomal gel. Conclusion: Proniosomal gel formulation was stable and could enhance skin delivery of etodolac because of excellent permeation capability of vesicular system.

Sign in / Sign up

Export Citation Format

Share Document