Development of biodegradable scaffolds loaded with vancomycin micropartricles for the treatment of osteomyelitis

In this present research work, the development of biodegradable scaffolds loaded with Vancomycin micropartricles was carried out for the treatment of Osteomyelitis. Characterization Vancomycin Loaded microparticles and evaluation of the microparticles loaded scaffolds and also to carry out In-vitro release studies. Vancomycin hydrochloride microparticles were prepared with the help of double emulsion method. HPMC and Polaxomer 407 has been taken as the main polymers for the preparation of the microparticles. Chitosan was taken as the major polymer for the preparation of scaffolds for its greater biocompatibility and biodegradability. The preparation was done with the help of the solvent casting method. The formulation was taken for further characterization and evaluation studies. Fourier-Transform Infrared Spectroscopy and Differential scanning calorimetry were carried out for the pure vancomycin drug, and the chitosan polymer X-ray diffraction was carried out to check the crystallinity of the prepared scaffolds. The particle size, zeta potential and polydispersity index for vancomycin loaded microparticles were found to be 577.0±102.5 nm, 1624 mv and 0.254. The maximum and sustained release rate of the drug was found to be 95.6±0.478, at 16th Hr. By taking all the reports, a conclusion can be drawn that, the formulated VLM biodegradable scaffolds will show burst release at the initial time of administration, which is essential for the wound healing activity and will be sustained throughout the process of treatment of osteomyelitis.

Download Full-text

Development and In-Vitro Evaluation of pH Responsive Polymeric Nano Hydrogel Carrier System for Gastro-Protective Delivery of Naproxen Sodium

Advances in Polymer Technology ◽

10.1155/2019/6090965 ◽

2019 ◽

Vol 2019 ◽

pp. 1-13

Author(s):

Rai Muhammad Sarfraz ◽

Muhammad Rouf Akram ◽

Muhammad Rizwan Ali ◽

Asif Mahmood ◽

Muhammad Usman Khan ◽

...

Keyword(s):

Drug Release ◽

Naproxen Sodium ◽

Research Work ◽

Entrapment Efficiency ◽

Gravimetric Analysis ◽

X Ray Diffraction ◽

Scanning Calorimetry ◽

Swelling Behaviour ◽

X Ray

Current research work was carried out for gastro-protective delivery of naproxen sodium. Polyethylene glycol-g-poly (methacrylic acid) nanogels was developed through free radical polymerization technique. Formulation was characterized for swelling behaviour, entrapment efficiency, Fourier transform infrared (FTIR) spectroscopy, Differential scanning calorimetry (DSC), and Thermal Gravimetric Analysis (TGA), Powder X-ray diffraction (PXRD), Zeta size distribution, and Zeta potential measurements, and in-vitro drug release. pH dependent swelling was observed with maximum drug release at higher pH. PXRD studies confirmed the conversion of loaded drug from crystalline to amorphous form while Zeta size measurement showed size reduction. On the basis of these results it was concluded that prepared nanogels proved an effective tool for gastro-protective delivery of naproxen sodium.

Download Full-text

FORMULATION AND EVALUATION OF SOLID LIPID NANOPARTICLES CONTAINING CAFFEINE TO TREAT CLINICAL MASTITIS

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2020.v13i7.37642 ◽

2020 ◽

pp. 72-78

Author(s):

AMRUTHA U ◽

SUSHMITHA B ◽

SHAIK RUBINA ◽

PADMINI IRIVENTI

Keyword(s):

Sustained Release ◽

Solid Lipid Nanoparticles ◽

Evaluation Studies ◽

In Vitro Release ◽

Lipid Nanoparticles ◽

Clinical Mastitis ◽

In Vitro Dissolution ◽

Scanning Calorimetry ◽

Solid Lipid

Objective: The objective of the present study was to formulate and evaluate caffeine loaded solid lipid nanoparticles (SLNs) in the treatment of clinical mastitis. Methodology: These were prepared by homogenization technique using cholesterol, tween 80, and chloroform as excipients. Preformulation studies such as ultraviolet spectrophotometry, Fourier transform infrared (FTIR), and differential scanning calorimetry (DSC) were performed for the drug. Entrapment efficiency and in vitro dissolution studies were carried out for prepared SLN’s and the optimum formulation (F2) was taken for further studies such as FTIR, DSC, scanning electron microscopy, particle size, and zeta potential analysis. Results: Obtained results stated that prepared SLNs are roughly spherical in nature and are in nanorange. These were incorporated in Carbopol gel and further evaluation studies such as pH, spreadability, viscosity, homogeneity, and in vitro drug diffusion studies were carried out. All the results obtained state that prepared nanogel has shown sustained release of drug. The antimicrobial study was carried out using Staphylococcus aureus and it was confirmed by appearance of the zone of inhibition. Conclusion: Nanogel that contains Caffeine SLNs with 1:2 ratio drug:lipid has shown good in vitro release. Sustained release of Caffeine drug till 12 h was achieved by delivering it in the form of nanogel.

Download Full-text

An Injectable Nano-Enabled Thermogel to Attain Controlled Delivery of p11 Peptide for the Potential Treatment of Ocular Angiogenic Disorders of the Posterior Segment

Pharmaceutics ◽

10.3390/pharmaceutics13020176 ◽

2021 ◽

Vol 13 (2) ◽

pp. 176

Author(s):

Lisa Claire du Toit ◽

Yahya Essop Choonara ◽

Viness Pillay

Keyword(s):

Polyethylene Glycol ◽

Polyacrylamide Gel Electrophoresis ◽

Sol Gel ◽

In Vitro Release ◽

Double Emulsion ◽

Controlled Delivery ◽

Retinal Cell ◽

Scanning Calorimetry ◽

Effective Prevention

This investigation focused on the design of an injectable nano-enabled thermogel (nano-thermogel) system to attain controlled delivery of p11 anti-angiogenic peptide for proposed effective prevention of neovascularisation and to overcome the drawbacks of the existing treatment approaches for ocular disorders characterised by angiogenesis, which employ multiple intravitreal injections of anti-vascular endothelial growth factor (anti-VEGF) antibodies. Synthesis of a polyethylene glycol-polycaprolactone-polyethylene glycol (PEG-PCL-PEG) triblock co-polymer was undertaken, followed by characterisation employing Fourier-transform infrared (FTIR) spectroscopy, nuclear magnetic resonance (NMR) spectroscopy and differential scanning calorimetry (DSC) to ascertain the chemical stability and integrity of the co-polymer instituted for nano-thermogel formulation. The p11 anti-angiogenic peptide underwent encapsulation within poly(lactic-co-glycolic acid) (PLGA) nanoparticles via a double emulsion solvent evaporation method and was incorporated into the thermogel following characterisation by scanning electron microscopy (SEM), zeta size and zeta-potential analysis. The tube inversion approach and rheological analysis were employed to ascertain the thermo-sensitive sol-gel conversion of the nano-thermogel system. Chromatographic assessment of the in vitro release of the peptide was performed, with stability confirmation via Tris-Tricine PAGE (Polyacrylamide Gel Electrophoresis). In vitro biocompatibility of the nano-thermogel system was investigated employing a retinal cell line (ARP-19). A nanoparticle size range of 100–200 nm and peptide loading efficiency of 67% was achieved. Sol-gel conversion of the nano-thermogel was observed between 32–45 °C. Release of the peptide in vitro was sustained, with maintenance of stability, for 60 days. Biocompatibility assessment highlighted 97–99% cell viability with non-haemolytic ability, which supports the potential applicability of the nano-thermogel system for extended delivery of peptide for ocular disorder treatment.

Download Full-text

Nanostructured-lipid carriers-Chitosan hydrogel beads carrier system for loading of resveratrol: A new method of topical application

Journal of Biomaterials Applications ◽

10.1177/08853282211053923 ◽

2022 ◽

pp. 088532822110539

Author(s):

Bi Wu ◽

Yang Li ◽

Yuan Y Li ◽

Zhi H Shi ◽

Xiao H Bian ◽

...

Keyword(s):

Skin Permeation ◽

Physical Stability ◽

In Vitro Release ◽

In Vitro Cytotoxicity ◽

Nanostructured Lipid Carriers ◽

X Ray Diffraction ◽

Scanning Calorimetry ◽

Chitosan Hydrogel ◽

Hydrogel Beads

The aim of this study was to develop nanostructured-lipid carriers (NLC) encapsulated by Chitosan hydrogel beads for the efficient topical carrier. Dynamic light scattering (DLS), X-ray diffraction (XRD), Differential scanning calorimetry (DSC), and attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR) were conducted to study the influence of the encapsulation on the characteristic of resveratrol-loaded NLC, and the results showed that there was no impact on resveratrol-loaded NLC. Chitosan hydrogel beads could significantly improve the physical stability of resveratrol-loaded NLC. In vitro release study revealed that resveratrol-loaded NLC-Chitosan hydrogel beads had a more significant sustained-release effect on resveratrol. In vitro transdermal studies suggested that the skin permeation of resveratrol was promoted by the effect of Chitosan hydrogel beads and increased resveratrol distribution in the skin. In vitro cytotoxicity showed that resveratrol-loaded NLC-Chitosan hydrogel beads did not exert a hazardous effect on L929 cells. Hence, NLC-Chitosan hydrogel beads might be a promising method for topical applications of resveratrol.

Download Full-text

Role of Aminated derivatives of Natural Gum in Release Modulating Matrix Systems of Losartan Potassium: Optimization of Formulation using Box-Behnken Design

Asian Journal of Pharmaceutical Research ◽

10.52711/2231-5691.2021.00015 ◽

2021 ◽

pp. 73-84

Author(s):

Shankar B. Kalbhare ◽

Vivek Kumar Redasani ◽

Mandar J. Bhandwalkar ◽

Rohit K. Pawar ◽

Avinash M. Bhagwat

Keyword(s):

Response Surface Methodology ◽

Response Surface ◽

Research Work ◽

In Vitro Release ◽

Kinetic Equations ◽

Matrix Tablets ◽

Losartan Potassium ◽

Burst Release ◽

Fenugreek Gum

The aim of the present research work was to systemically device a model of factors that would yield an optimized release modulating dosage form of an anti-hypertensive agent, losartan potassium, using response surface methodology by employing a 3-factor, 3-level Box-Behnken statistical design. Independent variables studied were the amount of the release retardant polymers – aminated fenugreek gum (X1), aminated tamarind gum (X2) and aminated xanthan gum (X3). The dependent variables were the burst release in 15 min (Y1), cumulative percentage release of drug after 60 min (Y2) and hardness (Y3) of the tablets with constraints on the Y2 = 31–35%. Statistical validity of the polynomials was established. In vitro release and swelling studies were carried out for the optimized formulation and the data were fitted to kinetic equations. The polynomial mathematical relationship obtained Y2=32.91-2.29X1-5.68X2-0.97X3+0.20X1X3-0.005X2X3-0.92X12-1.89X22 explained the main and quadratic effects, and the interactions of factors influencing the drug release from matrix tablets. The adjusted (0.9842) and predicted values (0.9600) of r2 for Y2 were in close agreement. Validation of the optimization study indicated high degree of prognostic ability of response surface methodology. The Box-Behnken experimental design facilitated the formulation and optimization of release modulating matrix systems of losartan potassium.

Download Full-text

Poly (2-hydroxyethylmethacrylate –co–methylmethacrylate)/Lignocaine Contact Lens Preparation, Characterization, and in vitro Release Dynamic

Polymers ◽

10.3390/polym11050917 ◽

2019 ◽

Vol 11 (5) ◽

pp. 917 ◽

Cited By ~ 2

Author(s):

Taieb Aouak ◽

Wassem Sharaf Saeed ◽

Nawaf M. Al-Hafi ◽

Abdel-Basit Al-Odayni ◽

Abdulaziz Ali Alghamdi ◽

...

Keyword(s):

Contact Lens ◽

Drug Carrier ◽

In Vitro Release ◽

Potential Candidate ◽

X Ray Diffraction ◽

Scanning Calorimetry ◽

Drug Carrier System ◽

Vitro Release ◽

Carrier Systems

2-hydroxyethyl methacrylate, methylmethacrylate, ethylene glycol dimethyl methacrylate, and lignocaine (drug) were mixed together and the monomers were copolymerized at 60 °C through a free radical polymerization in the presence of α,α′-Azoisobutyronitrile in tetrahydrofuran. A series of copolymer/drug composites with different monoacrylate monomer compositions were prepared by solvent evaporation and characterized by different methods such as nuclear magnetic resonance, differential scanning calorimetry, Fourier transform infrared, X-ray diffraction, and mechanical and optical testing. The water content in the copolymers and the cell viability test on the samples were also examined in this investigation. The results of the analyses of the properties of this drug-carrier system are promising, indicating that this material may be a potential candidate for contact lens applications. The release dynamic of this medication from the prepared drug-carrier systems was investigated in neutral pH media. The results obtained revealed that the diffusion of lignocaine through the copolymer matrix obeys the Fick model and the dynamic release can be easily controlled by the methyl methacrylate content in the copolymer.

Download Full-text

Nanoliposomes as Vehicles for Astaxanthin: Characterization, In Vitro Release Evaluation and Structure

Molecules ◽

10.3390/molecules23112822 ◽

2018 ◽

Vol 23 (11) ◽

pp. 2822 ◽

Cited By ~ 12

Author(s):

Li Pan ◽

Hongyan Wang ◽

Keren Gu

Keyword(s):

Lipid Bilayer ◽

Structural Changes ◽

In Vitro Release ◽

The Body ◽

Gravimetric Analysis ◽

X Ray Diffraction ◽

Scanning Calorimetry ◽

Fluorescence Measurements ◽

Water Dispersibility

Astaxanthin was encapsulated in nanoliposomes by a film dispersion-ultrasonic technique using soybean phosphatidyl choline. The astaxanthin-loaded nanoliposomes displayed advantages in the aspects of high encapsulation efficiency and less particle size with a remarkably homodisperse size distribution. Based on X-ray diffraction and differential scanning calorimetry the analysis, it has been demonstrated that there could be interactions of astaxanthin with the lipid bilayer, resulting in the forming of astaxanthin-loaded nanoliposomes. The thermal gravimetric analysis revealed that the thermal stability of astaxanthin after encapsulation in nanoliposomes was remarkably enhanced as compared to astaxanthin alone. Furthermore, encapsulation could greatly enhance the water dispersibility of astaxanthin. This study also confirmed that encapsulation of astaxanthin in nanoliposomes could be an effective way to supply astaxanthin continuously in the body. The effects of astaxanthin incorporation on structural changes of the liposomal membrane were investigated through steady-state fluorescence measurements. This study revealed that the incorporation of astaxanthin into the lipid bilayer decreased membrane fluidity, but increased micropolarity in the membrane within a certain range of astaxanthin concentrations. Additionally, it indicated that the encapsulation of astaxanthin in the lipid bilayer could be applied to modulate the structural properties of membranes.

Download Full-text

A Comparative Study of Acyclovir icroencapsulation by Novel Solvent Evaporation-Matrix Erosion and Spray Drying Techniques

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2012.5.1.6 ◽

2012 ◽

Vol 5 (1) ◽

pp. 1627-1637

Author(s):

J P Raval ◽

D R Naik

Keyword(s):

Spray Drying ◽

Ethyl Cellulose ◽

Drug Loading ◽

In Vitro Release ◽

Spherical Geometry ◽

Solvent Evaporation ◽

X Ray Diffraction ◽

Scanning Calorimetry ◽

Spray Dried

Designing and evaluating a multiparticulate controlled release dosage form, to increase the efficacy of acyclovir (a selective antiherpes agent). Spray drying technique for microsphere production is compared with novel solvent evaporation-matrix erosion technique for variable drug loading in different concentration of ethyl cellulose. The microspheres were characterized for physicochemical properties. The microspheres sizes were ranged from 7-25 μm. The spray dried microspheres had better encapsulation efficiency (up to 91%) compared to that of novel solvent evaporation-matrix erosion technique microspheres. Scanning electron microscopy confirmed spherical geometry due to high cross-linking density. Differential scanning calorimetry, Fourier-transform infrared spectroscopy and x-ray diffraction studies showed chemical stability and intactness of entrapped drug in the microspheres. In vitro release of acyclovir from spray dried microspheres continued for longer period compared to novel solvent evaporation-matrix erosion method. Overall, the release studies depended on the concentration of ethyl cellulose, extent of drug loading, and the technique used to prepare microspheres. Thus, marked retardation of drug release may provide a useful effective anti-retroviral drug therapy.

Download Full-text

Optimization and Formulation of Fucoxanthin-Loaded Microsphere (F-LM) Using Response Surface Methodology (RSM) and Analysis of Its Fucoxanthin Release Profile

Molecules ◽

10.3390/molecules24050947 ◽

2019 ◽

Vol 24 (5) ◽

pp. 947 ◽

Cited By ~ 2

Author(s):

Irwandi Jaswir ◽

Dedi Noviendri ◽

Muhammad Taher ◽

Farahidah Mohamed ◽

Fitri Octavianti ◽

...

Keyword(s):

Response Surface Methodology ◽

Surface Morphology ◽

Response Surface ◽

Release Kinetics ◽

In Vitro Release ◽

Double Emulsion ◽

Release Profile ◽

Burst Release ◽

Good Surface

Fucoxanthin has interesting anticancer activity, but is insoluble in water, hindering its use as a drug. Microencapsulation is used as a technique for improving drug delivery. This study aimed to formulate fucoxanthin-loaded microspheres (F-LM) for anticancer treatment of H1299 cancer cell lines and optimize particle size (PS) and encapsulation efficiency (EE). Using response surface methodology (RSM), a face centered central composite design (FCCCD) was designed with three factors: Polyvinylalcohol (PVA), poly(d,l-lactic-co-glycolic acid) (PLGA), and fucoxanthin concentration. F-LM was produced using a modified double-emulsion solvent evaporation method. The F-LM were characterized for release profile, release kinetics, and degradation pattern. Optimal F-LM PS and EE of 9.18 µm and 33.09%, respectively, with good surface morphology, were achieved from a 0.5% (w/v) PVA, 6.0% (w/v) PLGA, 200 µg/mL fucoxanthin formulation at a homogenization speed of 20,500 rpm. PVA concentration was the most significant factor (p < 0.05) affecting PS. Meanwhile, EE was significantly affected by interaction between the three factors: PVA, PLGA, and fucoxanthin. In vitro release curve showed fucoxanthin had a high burst release (38.3%) at the first hour, followed by a sustained release stage reaching (79.1%) within 2 months. Release kinetics followed a diffusion pattern predominantly controlled by the Higuchi model. Biodegradability studies based on surface morphology changes on the surface of the F-LM, show that morphology changed within the first hour, and F-LM completely degraded within 2 months. RSM under FCCCD design improved the difference between the lowest and highest responses, with good correlation between observed and predicted values for PS and EE of F-LM.

Download Full-text

Elaboration of Charged Poly(Lactic-co-Glycolic Acid) Microparticles for Effective Release of Tranexamic Acid

Polymers ◽

10.3390/polym12040808 ◽

2020 ◽

Vol 12 (4) ◽

pp. 808

Author(s):

Ming-Hsi Huang ◽

Shun-Ying Huang ◽

Yi-Xuan Chen ◽

Cheng-You Chen ◽

Yung-Sheng Lin

Keyword(s):

Tranexamic Acid ◽

Glycolic Acid ◽

Model Compound ◽

In Vitro Release ◽

Double Emulsion ◽

Scanning Calorimetry ◽

Solvent Evaporation Process ◽

Vitro Release ◽

Thermal Stability Of

In this study, tranexamic acid (TA) was used as a model compound to study the charge effect on the physicochemical properties of poly(lactic-co-glycolic acid) (PLGA) microparticles (MPs). Charged PLGA MPs were elaborated by the incorporation of a quaternary ammonium, cetyltrimethylammonium bromide (CTAB), during the double emulsion solvent evaporation process. Three TA-CTAB-carrying modes of PLGA MPs were designed in the CTAB-free (TA-MP), adsorption (TA-CTABAD), or encapsulation (TA-CTABEN) form. The obtained MPs were characterized by morphology and TA-MP affinity. The experiment revealed that the three prepared MPs were spherical and smooth, with pores on their surfaces. TA-CTABAD had a relatively narrow size distribution, compared with that of TA-MP and TA-CTABEN. The particle sizes of TA-MP, TA-CTABEN, TA-CTABAD were measured as 59 ± 17, 54 ± 20, and 19 ± 8 μm, respectively. The zeta potential of the three MPs was found to be in the order: TA-CTABAD > TA-CTABEN > TA-MP. Differential scanning calorimetry (DSC) indicated that the manufacturing process had no influence on the glass transition temperature of the MPs, which was close to 48 °C. Thermogravimetric analysis illustrated that the presence of CTAB slightly changed the thermal stability of PLGA MPs. In vitro release showed that TA-CTABAD exhibited faster TA release than TA-MP and TA-CTABEN in a basic environment (pH of 13), probably because of electrostatic attraction. At pH = 1, the release of TA from TA-CTABEN was faster than those from TA-MP and TA-CTABAD, probably because of electrostatic repulsion. However, the effect of electrostatic interaction was not significant at pH = 7.4.

Download Full-text