Remote-Controllable Bone-Targeted Delivery of Estradiol For the Treatment of Ovariectomy-Induced Osteoporosis in Rats

2021 ◽  
Author(s):  
Dehao Fu ◽  
Yuanyuan Guo ◽  
Yongwei Liu ◽  
Chen Shi ◽  
Tingting Wu ◽  
...  
Keyword(s):  
Particle Size ◽  
Bone Tissue ◽  
Targeted Delivery ◽  
Hormone Replacement ◽  
Plga Nanoparticles ◽  
Raw 264.7 Cells ◽  
Diffusion Method ◽  
Tissue Destruction ◽  
Trap 5B ◽  
Post Menopausal

Abstract BackgroundOsteoporosis (OP) is a systemic skeletal disease marked by bone mass reduction and bone tissue destruction. Hormone replacement therapy is an effective treatment for post-menopausal OP, but estrogen has poor tissue selectivity and severe side effects.ResultsIn this study, we constructed a poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs)-based drug delivery system to co-load 17β estradiol (E2) and iron oxide (Fe3O4) together, modified with alendronate (AL) to achieve bone targeting and realize a magnetically remote-controllable drug release. The NPs were fabricated through the emulsion solvent diffusion method. The particle size was approximately 200 nm while the encapsulation efficiency of E2 was 58.34 ± 9.21%. The NPs were found to be spherical with a homogenous distribution of particle size. The NPs showed good stability, good biocompatibility, high encapsulation ability of E2 and excellent magnetic properties. The NPs could be effectively taken up by Raw 264.7 cells and were effective in enriching drugs in bone tissue. The co-loaded NPs exposed to an external magnetic field ameliorated OVX-induced bone loss through increased BV/TV, decreased Tb.N and Tb.Sp, improved bone strength, increased PINP and OC, and downregulated CTX and TRAP-5b. The haematological index and histopathological analyses displayed the NPs had less side effects on non-skeletal tissues.ConclusionsThis study presented a remote-controlled release system based on bone-targeted multifunctional NPs and a new potential approach to bone-targeted therapy of OP.

scholarly journals Remote-controllable bone-targeted delivery of estradiol for the treatment of ovariectomy-induced osteoporosis in rats

2021 ◽  
Vol 19 (1) ◽  
Author(s):  
Yuanyuan Guo ◽  
Yongwei Liu ◽  
Chen Shi ◽  
Tingting Wu ◽  
Yongzhi Cui ◽  
...  
Keyword(s):  
Particle Size ◽  
Side Effects ◽  
Bone Tissue ◽  
Targeted Delivery ◽  
Hormone Replacement ◽  
Plga Nanoparticles ◽  
Raw 264.7 Cells ◽  
Diffusion Method ◽  
Tissue Destruction ◽  
Trap 5B

Abstract Background Osteoporosis (OP) is a systemic skeletal disease marked by bone mass reduction and bone tissue destruction. Hormone replacement therapy is an effective treatment for post-menopausal OP, but estrogen has poor tissue selectivity and severe side effects. Results In this study, we constructed a poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs)-based drug delivery system to co-load 17β estradiol (E2) and iron oxide (Fe3O4) together, modified with alendronate (AL) to achieve bone targeting and realize a magnetically remote-controllable drug release. The NPs were fabricated through the emulsion solvent diffusion method. The particle size was approximately 200 nm while the encapsulation efficiency of E2 was 58.34 ± 9.21%. The NPs were found to be spherical with a homogenous distribution of particle size. The NPs showed good stability, good biocompatibility, high encapsulation ability of E2 and excellent magnetic properties. The NPs could be effectively taken up by Raw 264.7 cells and were effective in enriching drugs in bone tissue. The co-loaded NPs exposed to an external magnetic field ameliorated OVX-induced bone loss through increased BV/TV, decreased Tb.N and Tb.Sp, improved bone strength, increased PINP and OC, and downregulated CTX and TRAP-5b. The haematological index and histopathological analyses displayed the NPs had less side effects on non-skeletal tissues. Conclusions This study presented a remote-controlled release system based on bone-targeted multifunctional NPs and a new potential approach to bone-targeted therapy of OP. Graphic abstract

Optimization of Curcuminoid-Loaded PLGA Nanoparticles Using Box-Behnken Statistical Design

2015 ◽  
Vol 33 ◽  
pp. 60-71 ◽  
Author(s):  
Praewpun Boonyasirisri ◽  
Ubonthip Nimmannit ◽  
Pranee Rojsitthisak ◽  
Settapon Bhunchu ◽  
Pornchai Rojsitthisak
Keyword(s):  
Particle Size ◽  
Curcuma Longa ◽  
Statistical Design ◽  
Entrapment Efficiency ◽  
Plga Nanoparticles ◽  
Molar Ratio ◽  
Diffusion Method ◽  
Alkaline Solutions ◽  
Loading Capacity ◽  
Spontaneous Emulsification

Curcuminoids are a mixture of phenolic compounds isolated from Curcuma longa L. (turmeric) rhizomes that possess antioxidant, anti-inflammatory, anti-Alzheimer and anticancer activities. However, curcuminoids have poor solubility in acid and neutral solutions, rapid decomposition in neutral and alkaline solutions, and low bioavailability that limits their use as therapeutic agents. To overcome these problems, statistical design for preparation and characterization of poly(D,L-lactide-co-glycolide) (PLGA) nanoparticles as a carrier for curcuminoids was evaluated in this study. The curcuminoid-loaded PLGA nanoparticles were prepared by a modified spontaneous emulsification solvent diffusion method using polyvinyl alcohol (PVA) as a stabilizer. The formulations were optimized using three-factor, three-level Box-Behnken experimental design. The independent variables in the formulations were the lactide/glycolide (LA/GA) molar ratio of PLGA (50:50 to 85:15), the curcuminoid concentration (2%-10%, w/v), and the PVA concentration (3%-7%, w/v). The dependent variables were particle size, loading capacity and entrapment efficiency. Statistical evaluation showed that the LA/GA molar ratio of PLGA and the curcuminoid and PVA concentrations all affected the characteristics of the PLGA nanoparticles. To achieve a minimum particle size and maximum loading capacity and entrapment efficiency, the optimal formulation of the curcuminoid-loaded PLGA nanoparticles had a LA/GA molar ratio of PLGA of 50:50, 10% (w/v) curcuminoids, and 3% (w/v) PVA. A sustainable in vitro release profile of curcuminoids was obtained from this optimal formulation.

Formulation and Evaluation of Mefloquine Hydrochloride Nanoparticles

2014 ◽  
Vol 7 (1) ◽  
pp. 2377-2386
Author(s):  
Dilip Kumar Gupta ◽  
B K Razdan ◽  
Meenakshi Bajpai
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Taste Masking ◽  
Diffusion Method ◽  
Drug Entrapment Efficiency ◽  
Resistant Strains ◽  
Vitro Release

The present study deals with the formulation and evaluation of mefloquine hydrochloride nanoparticles. Mefloquine is a blood schizonticidal quinoline compound, which is indicated for the treatment of mild-to-moderate acute malarial infections caused by mefloquine-susceptible multi-resistant strains of P. falciparum and P. vivax. The purpose of the present work is to minimize the dosing frequency, taste masking toxicity and to improve the therapeutic efficacy by formulating mefloquine HCl nanoparticles. Mefloquine nanoparticles were formulated by emulsion diffusion method using polymer poly(ε-caprolactone) with six different formulations. Nanoparticles were characterized by determining its particle size, polydispersity index, drug entrapment efficiency, drug content, particle morphological character and drug release. The particle size ranged between 100 nm to 240 nm. Drug entrapment efficacy was >95%. The in-vitro release of nanoparticles were carried out which exhibited a sustained release of mefloquine HCl from nanoparticles up to 24 hrs. The results showed that nanoparticles can be a promising drug delivery system for sustained release of mefloquine HCl.

Preparation, Characterization and In-vitro release of Piroxicam-loaded Solid Lipid Nanoparticles

2010 ◽  
Vol 3 (3) ◽  
pp. 1136-1146
Author(s):  
V K Verma ◽  
Ram A
Keyword(s):  
Electron Microscopy ◽  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Diffusion Method ◽  
Solid Lipid ◽  
Vitro Release

 Solid lipid nanoparticles (SLNs) of piroxicam where produced by solvent emulsification diffusion method in a solvent saturated system. The SLNs where composed of tripamitin lipid, polyvinyl alcohol (PVAL) stabilizer, and solvent ethyl acetate. All the formulation were subjected to particle size analysis, zeta potential, drug entrapment efficiency, percent drug loading determination and in-vitro release studies. The SLNs formed were nano-size range with maximum entrapment efficiency. Formulation with 435nm in particle size and 85% drug entrapment was subjected to scanning electron microscopy (SEM) and transmission electron microscopy (TEM) for surface morphology, differential scanning calorimetry (DSC) for thermal analysis and short term stability studies. SEM and TEM confirm that the SLNs are nanometric size and circular in shape. The drug release behavior from SLNs suspension exhibited biphasic pattern with an initial burst and prolong release over 24 h. 

Development and Evaluation of Particulate Microcarriers of Adapalene as a Topical Delivery System

2019 ◽  
Vol 9 (3) ◽  
pp. 222-233
Author(s):  
Divya D. Jain ◽  
Namita D. Desai
Keyword(s):  
Patient Compliance ◽  
Targeted Delivery ◽  
Ex Vivo ◽  
Acne Vulgaris ◽  
Drug Loading ◽  
Topical Therapy ◽  
Skin Irritation ◽  
Topical Delivery ◽  
Diffusion Method ◽  
Topical Gel

Background: Adapalene is a promising third generation retinoid used in the topical treatment of acne vulgaris. However, the major drawback associated with conventional topical therapy of Adapalene is the ‘retinoid reaction’ which is dose-dependent and characterized by erythema, scaling and burning sensation at the application sites. Microparticulate drug delivery can play a major role in reducing side effects and providing better patient compliance due to targeted delivery. Methods: Adapalene microparticles were prepared using quasi emulsion solvent diffusion method. The effects of formulation variables including polymer ratios, amounts of emulsifier, drug loading and process variables such as stirring time and speed on the physical characteristics of microparticles were investigated. The developed microparticles were characterized by DSC and SEM. Adapalene microparticles were incorporated into Carbopol 971 NF gel for ease of topical delivery. Results: Adapalene microparticulate topical gel showed sustained drug release over 8 hours in in vitro studies. The amount of drug retained in the rat skin during ex vivo studies was higher in the microparticulate topical gel (227.43 ± 0.83 µg/cm2) as compared to the marketed formulation (81.4 ± 1.11 µg/cm2) after 8 hours indicating localized and sustained drug action that can be useful in treating acne vulgaris. The safety of optimized Adapalene gel determined by skin irritation studies performed on Sprague Dawley rats showed no irritation potential. Conclusion: Microparticles can provide promising carrier systems to deliver Adapalene, improving patient compliance due to enhanced skin deposition, localized and sustained action with reduced associated irritant effects.

scholarly journals Dental Implant Site Drilling and Induced Morphological Changes Correlated with Temperature in Pig’s Rib Used as the Human Jaw Model

2021 ◽  
Vol 11 (6) ◽  
pp. 2493
Author(s):  
Karol Kirstein ◽  
Michalina Horochowska ◽  
Jacek Jagiełło ◽  
Joanna Bubak ◽  
Aleksander Chrószcz ◽  
...  
Keyword(s):  
Bone Tissue ◽  
Morphological Changes ◽  
Bone Destruction ◽  
Microscopic Investigation ◽  
In Vivo Studies ◽  
Drilling Speed ◽  
Tissue Destruction ◽  
Destruction Zone ◽  
Jaw Model

The bone tissue destruction during drilling is still one of the crucial problems in implantology. In this study, the influence of drilling speed, coolant presence, and its temperature on bone tissue was tested using swine rib as a biological model of human jaws. The same method of drilling (with or without coolant) was used in all tested samples. The microscopic investigation estimated the size of the destruction zone and morphology of bone tissue surrounding the drilling canal. The achieved results were statistically elaborated. The study proved that the optimal drilling speed was ca. 1200 rpm, but the temperature of the used coolant had no significant influence on provoked bone destruction. Simultaneously, the drilling system without coolant compared to this with coolant has statistical importance on drilling results. Further in vivo studies will verify the obtained results.

scholarly journals Effect of Chitosan Coating on PLGA Nanoparticles for Oral Delivery of Thymoquinone: In Vitro, Ex Vivo, and Cancer Cell Line Assessments

Coatings ◽  
2020 ◽  
Vol 11 (1) ◽  
pp. 6
Author(s):  
Sultan Alshehri ◽  
Syed Sarim Imam ◽  
Md Rizwanullah ◽  
Khalid Umar Fakhri ◽  
Mohd Moshahid Alam Rizvi ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Particle Size ◽  
Oral Delivery ◽  
Ex Vivo ◽  
Cancer Cell Line ◽  
Entrapment Efficiency ◽  
Plga Nanoparticles ◽  
Cancer Management ◽  
Mcf 7

In the present study, thymoquinone (TQ)-encapsulated chitosan- (CS)-coated poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles (NPs) were formulated using the emulsion evaporation method. NPs were optimized by using 33-QbD approach for improved efficacy against breast cancer. The optimized thymoquinone loaded chitosan coated Poly (d,l-lactide-co-glycolide) nanoparticles (TQ-CS-PLGA-NPs) were successfully characterized by different in vitro and ex vivo experiments as well as evaluated for cytotoxicity in MDA-MB-231 and MCF-7 cell lines. The surface coating of PLGA-NPs was completed by CS coating and there were no significant changes in particle size and entrapment efficiency (EE) observed. The developed TQ-CS-PLGA-NPs showed particle size, polydispersibility index (PDI), and %EE in the range between 126.03–196.71 nm, 0.118–0.205, and 62.75%–92.17%. The high and prolonged TQ release rate was achieved from TQ-PLGA-NPs and TQ-CS-PLGA-NPs. The optimized TQ-CS-PLGA-NPs showed significantly higher mucoadhesion and intestinal permeation compared to uncoated TQ-PLGA-NPs and TQ suspension. Furthermore, TQ-CS-PLGA-NPs showed statistically enhanced antioxidant potential and cytotoxicity against MDA-MB-231 and MCF-7 cells compared to uncoated TQ-PLGA-NPs and pure TQ. On the basis of the above findings, it may be stated that chitosan-coated TQ-PLGA-NPs represent a great potential for breast cancer management.

Targeted delivery of doxorubicin to A549 lung cancer cells by CXCR4 antagonist conjugated PLGA nanoparticles

2014 ◽  
Vol 88 (2) ◽  
pp. 529-538 ◽  
Author(s):  
Chuda Chittasupho ◽  
Kriengsak Lirdprapamongkol ◽  
Prartana Kewsuwan ◽  
Narong Sarisuta
Keyword(s):  
Lung Cancer ◽  
Cancer Cells ◽  
Targeted Delivery ◽  
Plga Nanoparticles ◽  
Lung Cancer Cells ◽  
Cxcr4 Antagonist ◽  
A549 Lung

Controlled Release Behaviors of Ketoprofen from Matrix Polymer of Chitosan and poly(ethylene glycol)

2013 ◽  
Vol 813 ◽  
pp. 399-402
Author(s):  
Chimsook Thitipha ◽  
Thitiphan Chimsook
Keyword(s):  
Particle Size ◽  
Controlled Release ◽  
Drug Release ◽  
Ethylene Glycol ◽  
Diffusion Method ◽  
Poly Ethylene Glycol ◽  
Matrix Polymer ◽  
Percentage Yield ◽  
Poly Ethylene ◽  
Composition Ratios

The aim of present work was to prepare floating microsphere of ketoprofen using matrix polymer of chitosan and poly (ethylene glycol) by solvent diffusion method. The floating microsphere of ketoprofen was prepared from matrix polymer of chitosan and poly (ethylene glycol) with various composition ratios and evaluated such as particle size, drug compatibility and drug release of microspheres. The scanning electron microscopy of microspheres confirmed their hollow structures with smooth surface. Formulation CPK 4 to CPK 6 exhibited the best controlled release pattern in ketoprofen. The concentration and size of poly (ethylene-glycol) affected the particle size, percentage yield and drug release of microspheres.

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