- The Drug Encapsulation Efficiency, in vitro Drug Release, Cellular Uptake and Cytotoxicity of Paclitaxel-Loaded Poly(Lactide)–Tocopheryl Polyethylene Glycol Succinate Nanoparticles

2014 ◽  
pp. 236-255
Author(s):  
Santosh G Gada ◽  
ANANDKUMAR Y. ◽  
C. MALLIKARJUN SETTY

Objective: The objective of this study was to design and evaluate controlled release mucoadhesive microspheres of lamivudine using mucoadhesive polymers and mucilage. Methods: Mucoadhesive microspheres of lamivudine were formulated by ionic gelation method. The response surface methodology was adapted for optimization of formulation using central composite design (CCD) for two factors at three levels each was employed to study the effect of independent variables, Sodium alginate-drumstick mucilage (X1) and calcium chloride (CaCl2) concentration (X2) on dependent variables, namely drug encapsulation efficiency (DEE) and particle size (PS). Optimized drumstick mucilage mucoadhesive microspheres of lamivudine were obtained by using numerical optimization of desirability approach. The observed microspheres were coincided well with the predicted values by the experimental design. Results: The microspheres formed were spherical in shape, and Particle size (PS) ranged between 681.63-941.57μm. Drug encapsulation efficiency (DEE) was ranged between 69.63-94.56 %. The drug release for an optimized formulation was 96.58 %. The mechanism of drug release from microspheres followed Korsemeyer’s-Peppas and exponential ‘n’ value was greater than 0.45, indicating the drug release was non-fickian i.e., swelling followed by erosion mechanism. Conclusion: This work suggests that mucoadhesive microspheres, an effective drug delivery system for lamivudine, can be prepared using drumstick mucilage in improving the bioavailability of the drug.


2019 ◽  
Vol 11 (2) ◽  
pp. 142-153
Author(s):  
Rutuja V. Deshmukh ◽  
Pavan Paraskar ◽  
S. Mishra ◽  
Jitendra Naik

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.


Bio-Research ◽  
2020 ◽  
Vol 18 (2) ◽  
Author(s):  
EB Onuigbo ◽  
C Anozie-Ikeanyi ◽  
NE Edeh ◽  
CO Eze ◽  
TH Gugu

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


2020 ◽  
Vol 11 (9) ◽  
pp. 557-571 ◽  
Author(s):  
Narendra ◽  
Abhishesh Kumar Mehata ◽  
Matte Kasi Viswanadh ◽  
Roshan Sonkar ◽  
Datta Maroti Pawde ◽  
...  

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.


2019 ◽  
Vol 49 ◽  
pp. 143-151 ◽  
Author(s):  
Muhammad Tahir Haseeb ◽  
Nisar Ul Khaliq ◽  
Soon Hong Yuk ◽  
Muhammad Ajaz Hussain ◽  
Sajid Bashir

2021 ◽  
Author(s):  
Tuğba Eren Böncü ◽  
Nurten Ozdemir

The aim of the study is to produce ampicillin trihydrate loaded PLA and PLA/PLGA polymeric nanofibers using HFIP as solvent via electrospinning. The effect of ampicillin trihydrate concentration (4-12%), the addition of PLGA and the amount of added PLGA (20-80%) on the spinnability of the solutions and morphology, average nanofiber diameter, encapsulation efficiency, in vitro drug release and mechanical properties of PLA and PLA/PLGA nanofibers were examined. All nanofibers have shown to have favorable encapsulation efficiency and mechanical properties. As the amount of ampicillin trihydrate increased and PLGA was added, nanofiber diameter increased while mechanical properties decreased. However, as the amount of added PLGA increased, a decrease in nanofiber diameter was observed. The increase in the drug amount caused an increase in the burst effect. The ideal drug concentration was determined to be 8% (F2), as it allows the prolonged and controlled drug release for up to 10 days. While in vitro drug release decreased with the addition of PLGA to PLA, it increased with the increasement of added PLGA to PLA. As a result of the study, it was concluded that the amount of the drug and the added PLGA concentration may affect the average nanofiber diameter, morphology, in vitro drug release and mechanical properties of the obtained electrospun PLA nanofibers.


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