In vitro drug release and antibacterial activity evaluation of silk fibroin coated vancomycin hydrochloride loaded poly (lactic-co-glycolic acid) (PLGA) sustained release microspheres

2022 ◽  
pp. 088532822110640
Author(s):  
Shengtang Li ◽  
Xuewen Shi ◽  
Bo Xu ◽  
Jian Wang ◽  
Peng Li ◽  
...  
Keyword(s):  
Drug Release ◽  
Encapsulation Efficiency ◽  
Glycolic Acid ◽  
Drug Loading ◽  
Burst Release ◽  
Plga Microspheres ◽  
In Vitro Drug Release ◽  
Initial Burst ◽  
Initial Burst Release

Currently, the treatment of osteomyelitis poses a great challenge to clinical orthopedics. The use of biodegradable materials combined with antibiotics provides a completely new option for the treatment of osteomyelitis. In this study, vancomycin hydrochloride (VANCO) loaded poly (lactic-co-glycolic acid) (PLGA) microspheres were prepared by a double emulsion solvent evaporation method, and the in vitro drug release behaviors of the drug loaded microspheres were explored after coating with different concentrations of silk fibroin (SF). Drug loading, encapsulation efficiency, Scanning electron microscopy, particle size analysis, Fourier transform infrared spectroscopy, hydrophilicity, in vitro drug release, and in vitro antibacterial activity were evaluated. The results showed that the drug loading of vancomycin loaded PLGA microspheres was (24.11 ±1.72)%, and the encapsulation efficiency was (48.21 ±3.44)%. The in vitro drug release indicated that the drug loaded microspheres showed an obvious initial burst release, and the drug loaded microspheres coated with SF could alleviate the initial burst release in varying degrees. It also can reduce the amount of cumulative drug release, and the effect of microspheres coated with 0.1% concentration of SF is the best. The time of in vitro drug release in different groups of drug loaded microspheres can be up to 28 days. The microspheres coated with (0.1%SF) or without (0%SF) SF showed a cumulative release of (82.50±3.51)% and (67.70±3.81)%,respectively. Therefore, the surface coating with SF of vancomycin loaded microspheres can alleviate the initial burst release, reduce the cumulative drug release, potentially prolong the drug action time, and improve the anti-infection effect.

Development and Evaluation of Guaifenesin Bilayer Tablet

2010 ◽  
Vol 3 (3) ◽  
pp. 1122-1128 ◽  
Author(s):  
Vijaya Kumar B ◽  
Prasad G ◽  
Ganesh B ◽  
Swathi C ◽  
Rashmi A ◽  
...  
Keyword(s):  
Drug Release ◽  
Angle Of Repose ◽  
Fickian Diffusion ◽  
In Vitro Dissolution ◽  
Burst Release ◽  
In Vitro Drug Release ◽  
Initial Burst ◽  
Drug Content ◽  
Bilayer Tablet

The objective of the present research was to develop a Bilayer tablet of guaifenesin (GBT) using superdisintegrant MCC and sodium starch glycolate for the fast release layer and metalose 90 SH and carbopol 934 for the sustaining layer. The guaifenesin SR granules of different formulation were evaluated for bulk density, tapped density, angle of repose, Carr’s index and Hausners ratio and results were found to be 0.460 ± 0.12 to 0.515 ± 0.03 gm/cm3 , 0.550 ±0.03 to 0.590 ±0.04 gm/cm3 , 19 ±0.01 to 26 ± 0.23, 13.72 ± 0.03 to 19.56 ± 0.04 & 1.137 to 1.196, respectively. The prepared bilayer tablets were evaluated for weight variation, hardness, friability, drug content and in vitro drug release. In vitro dissolution studies were carried out in a USP 24 apparatus I. The formulations gave an initial burst effect to provide the loading dose of the drug followed by sustained release for 12 h from the sustaining layer of matrix embedded tablets. In vitro dissolution kinetics followed the Higuchi model via a non-Fickian diffusion controlled release mechanism after the initial burst release. Stability studies conducted for optimized formulation did not show any change in physical appearance, drug content, matrix integrity and in vitro drug release. The results of the present study clearly indicated that GBT was a stable dosage form and a promising potential of the guaifenesin bilayer system as an alternative to the conventional dosage forms

Biodegradable Amphiphilic Tri-Block Copolymeric Nanoparticles for Controlled MTB Drug Delivery

2012 ◽  
Vol 584 ◽  
pp. 460-464 ◽  
Author(s):  
M Gajendiran ◽  
S. Balasubramanian
Keyword(s):  
Drug Release ◽  
Drug Loading ◽  
Powder Xrd ◽  
Burst Release ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Loading Efficiency ◽  
Release Studies ◽  
Drug Loading Efficiency

. A series of biodegradable amphiphilic tri-block copolymers (PLGA–PEG–PLGA) have been derived from the diblock copolymer poly (lactic–co–glycolic acid (PLGA)) and polyethylene glycol (PEG). The mycobacterium tuberculosis (MTB) drug pyrazinamide (PZA) loaded polymer nanoparticles (NPs) have been prepared by probe-sonication followed by w/o/w double emulsification technique. The copolymers have been characterized by FTIR and 1HNMR spectroscopic techniques, TG-DTA analysis, GPC analysis and powder XRD pattern. The MTB drug loaded polymeric NPs have been characterized by FESEM, powder XRD, HRTEM and XPS analysis. The drug loading efficiency, drug content and in vitro drug release studies have been carried out by spectrophotometry. The drug loading efficiency and drug content of triblock copolymeric NPs were higher than these of diblock copolymeric microparticles (MPs). The in vitro drug release studies indicate that the NPs exhibit initial burst release followed by controlled release of PZA for longer durations. The drug release kinetics mechanism has been evaluated by zero order, first order, Korsemeyer-Peppas (KP) and Higuchi models.

Solid Lipid Nanoparticles for Topical Delivery of Acitretin for the Treatment of Psoriasis by Design of Experiment

2020 ◽  
Vol 12 (2) ◽  
pp. 4474-4491
Author(s):  
Rajkumar Aland ◽  
Ganesan M ◽  
P. Rajeswara Rao ◽  
Bhikshapathi D. V. R. N.
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Tem Analysis ◽  
In Vitro Drug Release ◽  
Solid Lipid

The main objective for this investigation is to develop and optimize the solid lipid nanoparticles formulation of acitretin for the effective drug delivery. Acitretin loaded SLNs were prepared by hot homogenization followed by the ultrasonication using Taguchi’s orthogonal array with eight parameters that could affect the particle size and entrapment efficiency. Based on the results from the analyses of the responses obtained from Taguchi design, three different independent variables including surfactant concentration (%), lipid to drug ratio (w/w) and sonication time (s) were selected for further investigation using central composite design. The  lipid Dynasan-116, surfactant poloxomer-188 and co surfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, zeta potential, drug entrapment efficiency, in vitro drug release and stability. All parameters were found to be in an acceptable range. TEM analysis has demonstrated the presence of individual nanoparticles in spherical shape and the results were compatible with particle size measurements.  In vitro drug release of optimized SLN formulation (F2) was found to be 95.63 ± 1.52%, whereas pure drug release was 30.12 after 60 min and the major mechanism of drug release follows first order kinetics release data for optimized formulation (F2) with non-Fickian (anomalous) with a strong correlation coefficient (R2 = 0.94572) of Korsemeyer-Peppas model. The total drug content of acitretin gel formulation was found to 99.86 ± 0.012% and the diameter of gel formulation was 6.9 ± 0.021 cm and that of marketed gel was found to be 5.7 ± 0.06 cm, indicating better spreadability of SLN based gel formulation. The viscosity of gel formulation at 5 rpm was found to be 6.1 x 103 ± 0.4 x 103 cp. The release rate (flux) of acitretin across the membrane and excised skin differs significantly, which indicates about the barrier properties of skin. The flux value for SLN based gel formulation (182.754 ± 3.126 μg cm−2 h−1) was found to be higher than that for marketed gel (122.345 ± 4.786 μg cm−2 h−1). The higher flux and Kp values of SLN based gel suggest that it might be able to enter the skin easily as compared with marketed gel with an advantage of low interfacial tension of the emulsifier film that ensures an excellent contact to the skin. This topically oriented SLN based gel formulation could be useful in providing site-specific dermal treatment of psoriasis

Effect of Polymer Source on In Vitro Drug Release from PLGA Microspheres

2021 ◽  
pp. 120907
Author(s):  
Bo Wan ◽  
Janki V. Andhariya ◽  
Quanying Bao ◽  
Yan Wang ◽  
Yuan Zou ◽  
...  
Keyword(s):  
Drug Release ◽  
Plga Microspheres ◽  
In Vitro Drug Release

scholarly journals Formulation, Development and Evaluation of Ibuprofen Loaded Nano-transferosomal Gel for the Treatment of Psoriasis

2019 ◽  
pp. 1-8
Author(s):  
Marwa H. Abdallah ◽  
Amr S. Abu Lila ◽  
Md. Khalid Anwer ◽  
El-Sayed Khafagy ◽  
Muqtader Mohammad ◽  
...  
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Vesicle Size

The present work was aimed to develop a transferosomal gel of ibuprofen (IBU) for the amelioration of psoriasis like inflammation. Three formulation of IBU loaded transferosomes (TFs1-TFs3) were prepared using different proportions of lipid (phospholipon 90H) and surfactant (tween 80) and further evaluated for vesicle size, zeta potential (ZP), entrapment efficiency and in vitro drug release. The IBU loaded transferosomes (TFs2) was optimized with vesicle size (217±8.4 nm), PDI (0.102), ZP (-31.5±4.3 mV), entrapment efficiency (88.4±6.9%) and drug loading (44.2±2.9%). Further, the optimized IBU loaded transferosomes (TFs2) was incorporated into 1% carbopol 934 gel base and characterized for homogeneity, extrudability, viscosity and drug content. The in vivo pharmacodynamic study of gel exhibited reduction in psoriasis like inflammation in mice. The ibuprofen loaded transferosomal gel was successfully developed and has shown the potential to be a new therapy against psoriasis like inflammation.

scholarly journals Sodium Alginate Nanoparticles of Isoniazid: Preparation and Evaluation

2019 ◽  
Vol 11 (06) ◽  
Author(s):  
Sumit Kumar ◽  
Dinesh Chandra Bhatt
Keyword(s):  
Particle Size ◽  
Sodium Alginate ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Average Particle Size ◽  
Average Particle ◽  
In Vitro Drug Release ◽  
Ionotropic Gelation ◽  
Preparation And Evaluation

Fabrication and evaluation of the Isoniazid loaded sodium alginate nanoparticles (NPs) was main objective of current investigation. These NPs were engineered using ionotropic gelation technique. The NPs fabricated, were evaluated for average particle size, encapsulation efficiency, drug loading, and FTIR spectroscopy along with in vitro drug release. The particle size, drug loading and encapsulation efficiency of fabricated nanoparticles were ranging from 230.7 to 532.1 nm, 5.88% to 11.37% and 30.29% to 59.70% respectively. Amongst all batches studied formulation F-8 showed the best sustained release of drug at the end of 24 hours.

Development of Nateglinide Loaded Graphene Oxide-Chitosan Nanocomposites: Optimization by Box Behnken Design

2019 ◽  
Vol 11 (2) ◽  
pp. 142-153
Author(s):  
Rutuja V. Deshmukh ◽  
Pavan Paraskar ◽  
S. Mishra ◽  
Jitendra Naik
Keyword(s):  
Fourier Transform ◽  
Graphene Oxide ◽  
Electron Microscope ◽  
Drug Release ◽  
Sustained Release ◽  
Encapsulation Efficiency ◽  
In Vitro Drug Release ◽  
Box Behnken Design ◽  
X Ray

Background: Nateglinide is an antidiabetic drug having biological half-life 1.5 h which shows a concise effect. Graphene oxide along with chitosan can be used as a nanocarrier for sustained release of Nateglinide. Objective: To develop Nateglinide loaded graphene oxide-chitosan nanocomposites and to evaluate for different characterization studies. Methods: Graphene Oxide (GO) was synthesized by improved hummer’s method and drug-loaded Graphene oxide - chitosan nanocomposites were prepared. Box Behnken design was used to carry out experiments. The nanocomposites were characterized for encapsulation efficiency and drug release. Morphology was studied using field emission scanning electron microscope and transmission electron microscope. An interaction between drug, polymer and GO was investigated by Fourier transform infrared spectroscopy and X-ray diffractometer along with in vitro drug release study. Results: The statistical evaluation of the design showed linear and quadratic models which are significant models for encapsulation efficiency (R1 0.6883, 0.9473) and drug loading (R2 0.6785, 0.9336), respectively. Fourier transform infrared spectroscopy showed the compatibility of GO, Chitosan and Nateglinide. X-ray diffractometer reveals the change in degree of crystallinity of drug. FE-SEM and TEM images confirmed the distribution of the drug within the nanocomposites. Design expert reveals that the concentration of GO has great influence on encapsulation efficiency. In Vitro drug release showed the sustained release of drug over the period of 12 h. Conclusion: GO-Chitosan nanocomposites can be used as a sustained release carrier system for Nateglinide to reduce dose frequency of drug as well as its probable side effects.

scholarly journals PREPARATION, CHARACTERISATION AND EVALUATION OF ROPINIROLE HYDROCHLORIDE LOADED CONTROLLED RELEASE MICROSPHERES USING SOLVENT EVAPORATION TECHNIQUE

2018 ◽  
Vol 10 (6) ◽  
pp. 57
Author(s):  
Koyel Kar ◽  
R. N. Pal ◽  
N. N. Bala
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
Solvent Evaporation ◽  
In Vitro Drug Release ◽  
Aqueous Solvent ◽  
Evaporation Technique ◽  
Ropinirole Hydrochloride

Objective: The major objective of the research work was to design, characterise and evaluate controlled release microspheres of ropinirole hydrochloride by using non-aqueous solvent evaporation technique to facilitate the delivery of the drug at a predetermined rate for a specific period of time.Methods: Ropinirole hydrochloride microspheres were prepared by using different low-density polymers such as eudragit RL 100, eudragit RS 100 and ethylcellulose either alone or in combination with the help of non-aqueous solvent evaporation technique. All the formulated microparticles were subjected to various evaluation parameters such as particle size analysis, micrometric properties, drug entrapment efficiency, percentage drug loading, percentage yield and in vitro drug release study. The compatibility of the drug and polymers was confirmed by physical compatibility study, fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and x-ray diffraction study (XRD). The formation of the most optimized batch of the microsphere (F12) was confirmed by scanning electron microscopy (SEM), DSC, FTIR, and XRD. In vitro drug release study and in vitro drug release kinetics study of the formulated microspheres were also carried out.Results: Drug-polymer compatibility studies performed with the help of FTIR and DSC indicated that there were no interactions. Results revealed that non-aqueous solvent evaporation technique was a suitable technique for the preparation of microspheres as most of the formulations were discrete, free-flowing and spherical in shape with a good yield of 55.67% to 80.09%, percentage drug loading of 35.52% to 94.50% and percentage drug entrapment efficiency of 36.24% to 95.07%. Different drug-polymer ratios, as well as the combination of polymers, played a significant role in the variation of over-all characteristics of formulations. Based on the data of various evaluation parameters such as particle size analysis, percentage drug loading, percentage drug entrapment, percentage yield, rheological studies and in vitro drug release characteristics, formulation F12 was found to fulfil the criteria of ideal controlled release drug delivery system. F12 showed controlled release till the 14th hour (97.99%) and its in vitro release kinetics was best explained by zero-order kinetics and followed Korsemeyer-Pappas model (Non-Fickian mechanism). SEM of F12 revealed the formation of spherical structures. The FTIR study of F12 confirmed the stable nature of ropinirole in the drug-loaded microspheres. DSC and XRD patterns showed that ropinirole hydrochloride was dispersed at the molecular level in the polymer matrix.Conclusion: The controlled release microparticles were successfully prepared and from this study, it was concluded that the developed microspheres of ropinirole hydrochloride can be used for controlled drug release to improve the bioavailability and patient compliance and to maintain a constant drug level in the blood target tissue by releasing the drug in zero order pattern.

scholarly journals Chitosan-based nanoparticles sustenance and potentiation of the antibacterial effect of ampicillin against drug resistance among strains of Escherichia coli

Bio-Research ◽  
2020 ◽  
Vol 18 (2) ◽  
Author(s):  
EB Onuigbo ◽  
C Anozie-Ikeanyi ◽  
NE Edeh ◽  
CO Eze ◽  
TH Gugu
Keyword(s):  
Drug Resistance ◽  
Drug Release ◽  
Encapsulation Efficiency ◽  
Antibacterial Effect ◽  
Sodium Tripolyphosphate ◽  
Chitosan Nanoparticles ◽  
In Vitro Drug Release ◽  
E Coli ◽  
Ampicillin Trihydrate

The study seeks to evaluate nanoparticles based on chitosan for enhanced delivery of ampicillin in plasmid-mediated drug resistance. Serial dilutions of a mixed population of E. coli was plated on nutrient agar and streaked on Replica-plate 25 random colonies using MacConkey agar with or without ampicillin (100 µg/ml) daily for 96 h. Nanoparticles were prepared by cross-linking chitosan with sodium tripolyphosphate with ampicillin trihydrate adsorbed. Three different batches were prepared for optimization. The nanoparticles were optimized based on encapsulation efficiency, in vitro drug release, pH stability and microbiological assay using two laboratory strains of E. coli. Increased resistance to ampicillin due to possible plasmid transfer was established in vitro after 96 h. The encapsulation efficiency of the three batches was between 21-57 %. The drug release showed a burst effect and slow extended release over 8 h and reached a peak of about 19 % release at the 6 and 7 h in Batch A, B and C. The pH of the particles was stable over a period of 6 d. The nanoparticles containing only 0.075 mg of ampicillin dropped in an agar well plate inoculated with 1 ml of E. coli J62 lac pro trp hispFlac::Tn3 (AmpR) gave an IZD of ≥ 25 mm. Chitosan nanoparticles holds good potentials in potentiating the antibacterial effect of ampicillin against possible plasmid-mediated drug resistance

Formulation and in vitro evaluation of upconversion nanoparticle-loaded liposomes for brain cancer

2020 ◽  
Vol 11 (9) ◽  
pp. 557-571 ◽  
Author(s):  
Narendra ◽  
Abhishesh Kumar Mehata ◽  
Matte Kasi Viswanadh ◽  
Roshan Sonkar ◽  
Datta Maroti Pawde ◽  
...  
Keyword(s):  
Drug Release ◽  
Encapsulation Efficiency ◽  
Glioma Cells ◽  
C6 Glioma Cells ◽  
Upconversion Nanoparticles ◽  
Clinical Validation ◽  
In Vivo Evaluation ◽  
In Vitro Drug Release

Aim: This work focused on the development of transferrin-conjugated theranostic liposomes consisting of docetaxel (DXL) and upconversion nanoparticles for the diagnosis and treatment of gliomas. Materials & methods: Upconversion nanoparticles and docetaxel-loaded theranostic liposomes were prepared by a solvent injection method. Formulations were analyzed for physicochemical properties, encapsulation efficiency, drug release, elemental analysis, cytotoxicity and fluorescence. Results: The particle size was around 200 nm with spherical morphology and an encapsulation efficiency of up to 75.93%, was achieved for liposomes with an in vitro drug release of 71.10%. The IC50 values demonstrated enhanced cytotoxicity on C6 glioma cells with targeted liposomes in comparison with nontargeted liposomes. Conclusion: Prepared theranostic liposomes may be promising for clinical validation after an in vitro and in vivo evaluation on cell lines and animals, respectively.

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