scholarly journals Design of Targeted Flurbiprofen Biomimetic Nanoparticles for Management of Arthritis: In Vitro and In Vivo Appraisal

Pharmaceutics ◽  
2022 ◽  
Vol 14 (1) ◽  
pp. 140
Author(s):  
Hagar I. Mohamed ◽  
Amal H. El-Kamel ◽  
Ghada O. Hammad ◽  
Lamia A. Heikal
Keyword(s):  
Therapeutic Effect ◽  
Physicochemical Characterization ◽  
Entrapment Efficiency ◽  
In Vivo Studies ◽  
Histopathological Analysis ◽  
Biomimetic Nanoparticles ◽  
Rapid Clearance ◽  
Turbidimetric Assay

Flurbiprofen (FLUR) is a potent non-steroidal anti-inflammatory drug used for the management of arthritis. Unfortunately, its therapeutic effect is limited by its rapid clearance from the joints following intra-articular injection. To improve its therapeutic efficacy, hyaluronic acid-coated bovine serum albumin nanoparticles (HA-BSA NPs) were formulated and loaded with FLUR to achieve active drug targeting. NPs were prepared by a modified nano-emulsification technique and their HA coating was proven via turbidimetric assay. Physicochemical characterization of the selected HA-BSA NPs revealed entrapment efficiency of 90.12 ± 1.06%, particle size of 257.12 ± 2.54 nm, PDI of 0.25 ± 0.01, and zeta potential of −48 ± 3 mv. The selected formulation showed in-vitro extended-release profile up to 6 days. In-vivo studies on adjuvant-induced arthritis rat model exhibited a significant reduction in joint swelling after intra-articular administration of FLUR-loaded HA-BSA NPs. Additionally, there was a significant reduction in CRP level in blood as well as TNF-α, and IL-6 levels in serum and joint tissues. Immunohistochemical study indicated a significant decrease in iNOS level in joint tissues. Histopathological analysis confirmed the safety of FLUR-loaded HA-BSA NPs. Thus, our results reveal that FLUR loaded HA-BSA NPs have a promising therapeutic effect in the management of arthritis.

Formulation and In Vivo Evaluation of Mucoadhesive Micro-spheres of Rebamipide, a Mucoprotective Drug for GIT Disorders

2018 ◽  
Vol 11 (3) ◽  
pp. 4089-4097
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Kanteepan P
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
In Vivo Studies ◽  
Amino Acid Derivative ◽  
Release Mechanism ◽  
In Vivo Evaluation ◽  
In Vitro Drug Release ◽  
Percentage Yield

Rebamipide, an amino acid derivative of 2-(1H)-quinolinone, is used for mucosal protection, healing of gastroduodenal ulcers, and treatment of gastritis. The current research study aimed to develop novel gastro-retentive mucoadhesive microspheres of rebamipide using ionotropic gelation technique. Studies of micromeritic properties confirmed that microspheres were free flowing with good packability. The in vitro drug release showed the sustained release of rebamipide up to 99.23 ± 0.13% within 12 h whereas marketed product displayed the drug release of 95.15 ± 0.23% within 1 h. The release mechanism from microspheres followed the zero-order and Korsmeyer-Peppas (R2 = 0.915, 0.969), respectively. The optimized M12 formulation displayed optimum features, such as entrapment efficiency 97%, particle size 61.94 ± 0.11 µm, percentage yield 98%, swelling index 95% and mucoadhesiveness was 97%. FTIR studies revealed no major incompatibility between drug and excipients. SEM confirmed the particles were of spherical in shape. Optimized formulation (M12) were stable at 40°C ± 2°C/75% RH ± 5% RH for 6 months. In vivo studies were performed and kinetic parameters like Cmax, Tmax, AUC0-t, AUC0-∞, t1/2, and Kel  were calculated. The marketed product Cmax (3.15 ± 0.05 ng/mL) was higher than optimized formulation (2.58 ± 0.03 ng/mL). The optimized formulation AUC0-t (15.25 ± 1.14 ng.hr/mL), AUC0-∞ (19.42 ± 1.24 ng.hr/mL) was significantly higher than that of marketed product AUC0-t (10.21 ± 1.26 ng.hr/mL) and AUC0-∞ (13.15 ± 0.05 ng.hr/mL). These results indicate an optimized formulation bioavailability of 2.5-fold greater than marketed product.  

Formulation of sustained-release microspheres of cefixime with enhanced oral bioavailability and antibacterial potential

2019 ◽  
Vol 10 (12) ◽  
pp. 769-782
Author(s):  
Karan Razdan ◽  
Nikhil S Sahajpal ◽  
Kuldeep Singh ◽  
Harmanpreet Singh ◽  
Harjeet Singh ◽  
...  
Keyword(s):  
Sustained Release ◽  
Entrapment Efficiency ◽  
Salmonella Typhi ◽  
In Vivo Studies ◽  
In Vitro Drug Release ◽  
Dosing Frequency ◽  
Twofold Decrease ◽  
Antibacterial Potential

Aim: The present work focused on the development of sustained-release microsphere formulation of cefixime to provide reduction in dosing frequency, improved antibacterial activity and patient compliance. Methodology & results: Microspheres were prepared by modified emulsion solvent evaporation method and evaluated by in vitro and in vivo studies. Optimized formulation (FK-07) was found to have entrapment efficiency of 81.12 ± 0.93% and particle size of 166.82 ± 0.86 μm. FK-07 sustained release up to 24 h as demonstrated by in vitro drug release and in vivo pharmacokinetic study in rats. FK-07 showed approximately twofold increase in bioavailability and twofold decrease in MIC90 value against Escherichia coli, Klebsiella pneumoniae and Salmonella typhi in comparison to marketed formulation. Conclusion: Sustaining the release of cefixime using microspheres enhanced its bioavailability, antibacterial efficacy and will help in reducing its dosing frequency.

Development and Characterization of a Clobetasol Propionate Nanostructured Lipid Carrier-based Gel for the Treatment of Plaque Psoriasis

2020 ◽  
Vol 13 ◽  
Author(s):  
Ankita Dadwal ◽  
Neeraj Mishra ◽  
Raj Kumar Narang
Keyword(s):  
Skin Permeation ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Homogenization Method ◽  
Clobetasol Propionate ◽  
In Vivo Studies ◽  
Nanostructured Lipid Carrier ◽  
Safe Delivery

Background: Psoriasis is an autoimmune disease of the skin with lapsing episodes of hyperkeratosis, irritation, and inflammation. Numerous traditional and novel drug delivery systems have been used for better penetration through psoriatic barrier cells and also for retention in the skin. As there is no effective remedy for better penetration and retention is there because of the absence of an ideal carrier for effective and safe delivery of antipsoriatic drugs. Objectives: The main objective of this project is to develop Squalene integrated NLC based carbopol 940 gel to create a local drug depot in skin for improved efficacy against psoriasis. Methods: Homogenization method is used for the formulation of Nanostructured Lipid Carrier and were characterized on the basis of size, entrapment efficiency, polydispersity index (PDI), viscosity, spreadability, DSC, zeta potential, % in vitro release, in vitro skin permeation and retention studies, physical storage stability studies and in vivo studies can use other alternative models for induction of psoriasis by severe redness, swelling macroscopically and microvascular dilation edema lasting for 10 days. Further histopathology study was done to basses of changes in the skin. Conclusion: The optimized formulation of nanostructured lipid carrier-based gel has shown significant sustained release of clobetasol propionate. Further, this formulation has also shown retention in skin because of squalene as it is sebum derived lipid show affinity towards the sebaceous gland.

scholarly journals Garcinol loaded vitamin E TPGS emulsified PLGA nanoparticles: preparation, physicochemical characterization, in vitro and in vivo studies

2017 ◽  
Vol 7 (1) ◽  
Author(s):  
Raghuvir H. Gaonkar ◽  
Soumya Ganguly ◽  
Saikat Dewanjee ◽  
Samarendu Sinha ◽  
Amit Gupta ◽  
...  
Keyword(s):  
Vitamin E ◽  
Physicochemical Characterization ◽  
Plga Nanoparticles ◽  
In Vivo Studies ◽  
Vitamin E Tpgs

Development of a novel keratin dressing which accelerates full-thickness skin wound healing in diabetic mice: In vitro and in vivo studies

2018 ◽  
Vol 33 (4) ◽  
pp. 527-540 ◽  
Author(s):  
Marek Konop ◽  
Joanna Czuwara ◽  
Ewa Kłodzińska ◽  
Anna K Laskowska ◽  
Urszula Zielenkiewicz ◽  
...  
Keyword(s):  
Wound Healing ◽  
Wound Dressing ◽  
Healing Process ◽  
Skin Wound ◽  
In Vivo Studies ◽  
Histopathological Analysis ◽  
Full Thickness ◽  
Impaired Wound Healing

Impaired wound healing is a major medical problem in diabetes. The objective of this study was to determine the possible application of an insoluble fraction of fur-derived keratin biomaterial as a wound dressing in a full thickness surgical skin wound model in mice ( n = 20) with iatrogenically induced diabetes. The obtained keratin dressing was examined in vitro and in vivo. In vitro study showed the keratin dressing is tissue biocompatible and non-toxic for murine fibroblasts. Antimicrobial examination revealed the keratin dressing inhibited the growth of S. aureus and E. coli. In vivo studies showed the obtained dressing significantly ( p < 0.05) accelerated healing during the first week after surgery compared to control wounds. Keratin dressings were incorporated naturally into granulation and regenerating tissue without any visible signs of inflammatory response, which was confirmed by clinical and histopathological analysis. It is one of the first studies to show application of insoluble keratin proteins and its properties as a wound dressing. The obtained keratin dressing accelerated wound healing in mice with iatrogenically induced diabetes. Therefore, it can be considered as a safe and efficient wound dressing. Although future studies are needed to explain the molecular mechanism behind fur-derived keratin effect during the multilayer wound healing process, our findings may open the way for a new class of insoluble fur keratin dressings in chronic difficult to heal wounds treatment.

Development of Polymeric Nanocarriers for Brain Targeted Delivery of Atorvastatin: A Quality-By-Design Approach

2020 ◽  
Vol 10 (2) ◽  
pp. 149-158
Author(s):  
Guilherme A.G. Martins ◽  
Fabio S. Murakami ◽  
Mauro S. Oliveira ◽  
Ana F. Furian ◽  
Helen Treichel ◽  
...  
Keyword(s):  
Quality By Design ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Physicochemical Characteristics ◽  
In Vivo Studies ◽  
Mean Size ◽  
Release Study ◽  
Vitro Release

Objective: Atorvastatin (ATV) is effective in reducing total cholesterol and low-density lipoprotein levels. Furthermore, it produces pleiotropic effects in neurodegenerative conditions such as Parkinson's, Alzheimer's, and epilepsy. However, due to the effective defense system of the central nervous system (CNS), the development of new medicines for clinical conditions has proven difficult. In this context, nanotechnology was applied as a promising solution to promote drug vectorization to the brain. Methods: The solvent emulsification-diffusion method was used to develop nanoparticles (NPs) based on polylactic acid and coated with polysorbate 80 containing ATV. Quality-by-Design (QbD) was used in the optimization of nanoparticles production through the application of the experimental design Box-Behnken Design. Results: After optimizing the independent factors including sonication time, surfactant concentration and surfactant volume, the NPs presented physicochemical characteristics such as entrapment efficiency of 86.4 ± 2.4%, mean size of 225.2 ± 4.8 nm, and zeta potential of -14.4 ± 0.36 mV. In the in vitro release study, approximately 20% of the encapsulated ATV was released. Conclusion: The application of QbD was very useful in demonstrating its applicability in the nanotechnological pharmaceutical area for controlling and predicting the influence of the variables in the production of NPs. The NPs developed in this study presented adequate physicochemical characteristics, which is promising for future in vivo studies. The physicochemical characteristics included entrapment efficiency of 86.4 ± 2.4%, mean size of 225.2 ± 4.8 nm, and zeta potential of -14.4 ± 0.36 mV. In the in vitro release study, approximately 20% of the encapsulated ATV was released. The application of QbD was very useful in demonstrating its applicability in the nanotechnological pharmaceutical area for controlling and predicting the influence of the variables in the production of NPs. The NPs developed in this study presented adequate physicochemical characteristics, which is promising for future in vivo studies.

Chemotherapeutic potential of L-carnosine from stimuli-responsive magnetic nanoparticles against breast cancer model

Nanomedicine ◽  
2020 ◽  
Vol 15 (9) ◽  
pp. 891-911
Author(s):  
Ragwa M Farid ◽  
Passent M E Gaafar ◽  
Heba A Hazzah ◽  
Maged W Helmy ◽  
Ossama Y Abdallah
Keyword(s):  
Magnetic Nanoparticles ◽  
Targeted Delivery ◽  
Physicochemical Characterization ◽  
Tumor Model ◽  
Entrapment Efficiency ◽  
In Vitro Cytotoxicity ◽  
Scanning Calorimetry ◽  
Chemotherapeutic Activity

Aim: L-carnosine-coated magnetic nanoparticles (CCMNPs) were developed to enhance chemotherapeutic activity of carnosine-dipeptide. Materials & methods: Surface grafting of MNPs with carnosine was contended by differential scanning calorimetry, infrared spectroscopy and x-ray diffraction. Physicochemical characterization and in vitro cytotoxicity on MCF-7 cell line was carried out. In vivo chemotherapeutic activity and toxicity was assessed by an Ehrlich Ascites tumor model. Results: CCMNPs possessed monodispersed size (120 nm), ζ (-27.3 mV), magnetization (51.52 emu/g) and entrapment efficiency (88.3%) with sustained release rate. CCMNPs showed 2.3-folds lower IC50 values compared with carnosine solution after 48 h. Targeted CCMNPs were specifically accumulated in tumor showing significant reduction in tumor size with no systemic toxicity. Significant reduction in VEGF and cyclin D1 levels were observed. Conclusion: The developed system endowed with responsiveness to an external stimulus can represent a promising magnetically targeted delivery system for carnosine site specific delivery.

scholarly journals PLGA nanoparticles for the oral delivery of nuciferine: preparation, physicochemical characterization and in vitro/in vivo studies

Drug Delivery ◽  
2017 ◽  
Vol 24 (1) ◽  
pp. 443-451 ◽  
Author(s):  
Ying Liu ◽  
Xin Wu ◽  
Yushuai Mi ◽  
Bimeng Zhang ◽  
Shengying Gu ◽  
...  
Keyword(s):  
Oral Delivery ◽  
Physicochemical Characterization ◽  
Plga Nanoparticles ◽  
In Vivo Studies

scholarly journals Recent strategies in nanodelivery systems for natural products: a review

2021 ◽  
Author(s):  
Giulia Vanti
Keyword(s):  
Natural Products ◽  
Water Solubility ◽  
Molecular Size ◽  
Structural Diversity ◽  
In Vivo Studies ◽  
Biological Targets ◽  
Routes Of Administration ◽  
Rapid Clearance

AbstractNatural products are major molecules for drug discovery due to their structural diversity and their interaction with various biological targets, yet their clinical application is limited by poor water solubility or low lipophilicity, inappropriate molecular size, low dissolution rate and permeation, instability, high metabolic rate and rapid clearance. These issues can be solved by nanomedicine, by improving bioavailability and therapeutic efficacy. Here we review nanocarriers made of polymer or lipid constituents. Specifically, we describe the technological characteristics of each nanosystem, with examples of application to single natural constituents or plant extracts, and possible routes of administration. We report in vitro and in vivo studies and we conclude with the potential advantages of nanodelivery systems in terms of increased stability and solubility, improved biodistribution and efficacy, reduced adverse effects and toxicity.

scholarly journals Preparation and Characterization of Silymarin-Conjugated Gold Nanoparticles with Enhanced Anti-Fibrotic Therapeutic Effects against Hepatic Fibrosis in Rats: Role of MicroRNAs as Molecular Targets

Biomedicines ◽  
2021 ◽  
Vol 9 (12) ◽  
pp. 1767
Author(s):  
Abdullah Saad Abdullah ◽  
Ibrahim El Tantawy El Sayed ◽  
Abdel Moneim A. El-Torgoman ◽  
Noweir Ahmad Alghamdi ◽  
Sami Ullah ◽  
...  
Keyword(s):  
Gold Nanoparticles ◽  
Hepatic Fibrosis ◽  
Entrapment Efficiency ◽  
In Vivo Studies ◽  
Therapeutic Effects ◽  
Related Factor ◽  
Serum Samples ◽  
Hepatic Expression

Background: The main obstacles of silymarin (SIL) application in liver diseases are its low bioavailability, elevated metabolism, rapid excretion in bile and urine, and inefficient intestinal resorption. The study aimed to synthesize and characterize silymarin-conjugated gold nanoparticles (SGNPs) formulation to improve SIL bioavailability and release for potentiating its antifibrotic action. Methods: Both SGNPs and gold nanoparticles (GNPs) were prepared and characterized using standard characterization techniques. The improved formulation was assessed for in vitro drug release study and in vivo study on rats using CCl4 induced hepatic fibrosis model. SIL, SGNPs, and GNPs were administered by oral gavage daily for 30 days. At the end of the study, rats underwent anesthesia and were sacrificed, serum samples were collected for biochemical analysis. Liver tissues were collected to measure the genes and microRNAs (miRNAs) expressions. Also, histopathological and immunohistochemistry (IHC) examinations of hepatic tissues supported these results. Results: The successful formation and conjugation of SGNPs were confirmed by measurements methods. The synthesized nanohybrid SGNPs showed significant antifibrotic therapeutic action against CCl4-induced hepatic damage in rats, and preserved normal body weight, liver weight, liver index values, retained normal hepatic functions, lowered inflammatory markers, declined lipid peroxidation, and activated the antioxidant pathway nuclear factor erythroid-2-related factor 2 (NRF2). The antifibrotic activities of SGNPs mediated through enhancing the hepatic expression of the protective miRNAs; miR-22, miR-29c, and miR-219a which results in suppressed expression of the main fibrosis mediators; TGFβR1, COL3A1, and TGFβR2, respectively. The histopathology and IHC analysis confirmed the anti-fibrotic effects of SGNPs. Conclusions: The successful synthesis of SGNPs with sizes ranging from 16 up to 20 nm and entrapment efficiency and loading capacity 96% and 38.69%, respectively. In vivo studies revealed that the obtained nano-formulation of SIL boosted its anti-fibrotic effects.

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