scholarly journals Chitosan Nanoparticles as a Percutaneous Drug Delivery System for Hydrocortisone

2012 ◽  
Vol 2012 ◽  
pp. 1-11 ◽  
Author(s):  
Haliza Katas ◽  
Zahid Hussain ◽  
Tay Chai Ling

Hydrocortisone (HC) has formed the mainstay for the management of atopic dermatitis. Hence, HC-loaded chitosan nanoparticles were prepared by ionic crosslinking of high, low molecular weight chitosan (HMwt, LMwt CS) and N-trimethyl chitosan (TMC) with tripolyphosphate. HC loading into CS nanoparticles was confirmed by FT-IR. The particle size of HC-loaded HMwt, LMwt, and TMC nanoparticles was increased from243±12,147±11,and124±9 nm to337±13,222±14,and195±7 nm, respectively, by increasing the pH of CS solution. Their respective zeta potential and entrapment efficiency (EE) were significantly decreased by increasing the pH of CS solution. The swelling ratios of HC loaded HMwt, LMwt, and TMC NPs were increased when the pH of incubating media (PBS) was increased. The same increasing trend was observed in particle size and EE of HC loaded as the CS concentration was increased. The HC loaded CS NPs were generally nonspherical.In-vitropermeation studies showed that HC was efficiently released from the CS NPs in QV cream while in aqueous cream CS NPs provided a sustained release for HC. Thus, it is anticipated that CS NPs are the promising delivery system for anti-inflammatory drugs.

Author(s):  
Tumpa Sarkar ◽  
Abdul Baquee Ahmed

ABSTRACTObjectives: To meet the above aim the following objectives are undertaken: (1) Preparation of paclitaxel (PTX) loaded nanoparticles by differenttechniques, (2) In-vitro evaluations of the drug loaded nanoparticles and selection of optimized batch.Methods: PTX loaded chitosan nanoparticles were prepared by Ionic-crosslinking technique. In this technique, chitosan was dissolved in 0.25%v/vacetic acid solution. To this above solution 0.84%v/v, glutaraldehyde solution was added dropwise under high-speed homogenizer at 17000 rpm for1 hr.Result: Particle size of prepared nanoparticle formulations was found to be 345.175±5.66-815.125±8.355 nm with low PDI between 0.456. Themaximum entrapment of drug was found to be 88.57±2.533% with formulation F5. In-vitro release studies of the F5 formulation showed 57.8±1.735%release of drug after 24 hrs.Conclusion: The prepared nanoparticles were evaluated for its particle size, zeta potential, drug entrapment efficiency, in-vitro drug release study,and surface morphology studies by scanning electron microscopy. The results of Fourier transform infrared studies of 1:1 physical mixture of drug andexcipients confirmed the absence of incompatibility. Thus, the study concludes that PTX loaded nanoparticles were developed successfully by ioniccrosslinking method, which is expected to enhance the oral bioavailability of PTX.Keywords: Paclitaxel, Nanoparticles, Chitosan, Ionic-crosslinking, In-vitro release.


Author(s):  
S. PATHAK ◽  
S. P. VYAS ◽  
A. PANDEY

Objective: The objective of the present study was to develop, optimize, and evaluate Ibandronate-sodium loaded chitosan nanoparticles (Ib-CS NPs) to treat osteoporosis. Methods: NPs were prepared by the Ionic gelation method and optimized for various parameters such as the effect of concentration of chitosan, sodium tripolyphosphate (TPP), and pH effect on particle size polydispersity index (PDI), zeta potential, and entrapment efficiency. The prepared nanoparticles were characterized using particle size analyzer (DLS), transmission electron microscopy (TEM), scanning electron microscopy (SEM), and Fourier-Transform Infrared spectroscopy (FTIR).  Results: Formulated NPs were obtained in the average nano size in the range below 200 nm in TEM, SEM, and DLS studies. The particle size and encapsulation efficiency of the optimized formulation were 176.1 nm and 63.28%, respectively. The release profile of NPs was depended on the dissolution medium and followed the First-order release kinetics. Conclusion: Bisphosphonates are the most commonly prescribed drugs for treating osteoporosis in the US and many other countries, including India. Ibandronate is a widely used anti-osteoporosis drug, exhibits a strong inhibitory effect on bone resorption performed by osteoclast cells. Our results indicated that Ibandronate sodium-loaded chitosan nanoparticles provide an effective medication for the treatment of osteoporosis.


2011 ◽  
Vol 282-283 ◽  
pp. 539-544 ◽  
Author(s):  
Jia Lei Li ◽  
Yuan Gang Zu ◽  
Xiu Hua Zhao ◽  
Zhi Gang An ◽  
Xiao Yu Sui ◽  
...  

Epigallocatechin-3-gallate (EGCG), a principal polyphenolic, which is most abundant and active component in tea. It is considered key to these healthful qualities. However, EGCG used in clinical application which is still shortcomings of short half-life and low bioavailability. Chitosan (CS) has been widely used in pharmaceutical and medical areas, particularly for its potential in the development of controlled release drug delivery systems due to its well properties. In this study, we prepared EGCG-loaded chitosan nanoparticles by ionic polymeric method using sodium tripolyphosphate(TPP) as ionic polymeric agent successfully. Results controlled conditions (concentration of CS, 2 mg/mL; pH = 5.4; volume of TPP(0.5 mg/mL), 6.6 mL; amount of EGCG, 15 mg; ionic polymeric time, 24 h at room temperature (0.5 mL/min))volume of TPP(0.5 mg/mL), 6.6 mL; amount of EGCG, 15 mg; ionic polymeric time, 24 h at room temperature (0.5 mL/min)) for entrapment efficiency, loading efficiency, mean particle size and Zeta potential, were found to be 62.3 %, 33.8 %, 141.5 ± 0.4 nm and -31.21 ± 0.54 mV, respectively, and CS-EGCG-NPS have well property of sustained release.


Author(s):  
Anupriya Anand ◽  
Bharadhwaj Ramesh Iyer ◽  
Chandrasekar Ponnusamy ◽  
Rajesh Pandiyan ◽  
Abimanyu Sugumaran

Aim: The present research work discussed the preparation of lomustine loaded with chitosan nanoparticles (LNCp) by ionic gelation method with homogenization using the design on experiments by Box-Behnken design. Methods: The nanoparticles are evaluated by particle size, zeta potential, surface morphology, drug content, entrapment efficiency and in-vitro drug release. Results: The FT-IR results support that drug have no interaction with excipients, which are used in the preparation of nanoparticle. The particle size, drug content and encapsulation efficiency of the developed nanoparticles ranged from 190 to 255 nm, 80.88% to 94.02%, and 77.12 to 88.74%, respectively. The drug release rate is diffusion-controlled over 8 hours. The F-value for all of the responses shows that the models are significant. The p-value, less than 0.05 for all the responses reveals the significance of the models. Graphical optimisation is done by desirability plot and overlay plot, which contains optimal values of independent variables with the desirability of 1. Conclusion: In conclusion, the results suggested that the optimised lomustine loaded chitosan nanoparticles are useful for brain targeting hence hold the potential for further research and clinical application.


2021 ◽  
Author(s):  
Cheran K ◽  
Udaykumar B Bolmal ◽  
Archana S Patil ◽  
Umashri A Kokatanur ◽  
Rajashree S Masareddy

Abstract Background: The goal of this study was to develop a gastro retentive floating drug delivery system that would improve site specific activity, patient compliance and therapeutic efficacy.Methodology: Floating microspheres of Miglitol were formulated by double emulsion method using ethyl cellulose and eudragit E100 different weight ratio and PVA as an emulsifier. It has been prepared with respect quantity of polymer concentration and stirring speed to evaluate for % buoyancy, drug entrapment efficiency, particle size drug release rate. Result: The percent of buoyancy, drug entrapment efficiency, particle size, and percentage yield were increased with increase the polymer mixture concentration. Among all formulation batches, F6 showed acceptable results drug entrapment efficiency (86.57%) and buoyancy (94.25%). F10 formulation was prepared to check the predicted and actual factors and compared with optimized formulation F6. The drug release was increased as the polymer concentration was decrease. The kinetic model zero order had the highest regression coefficient value, it was described as a sustained release dosage form. According to ICH guideline accelerated stability studies of F6 and F10 formulations were conducted for 90 days. After 90 days buoyancy and in vitro drug release was performed and the results were F6 and F10 buoyancy was found to be 88.21%, 87.22% and in vitro drug release was found to be 62.87%, 63.51%. Conclusion: The present study, showed compatibility of drug with polymers by FTIR in formulation. Floating microsphere of Miglitol was prepared by double emulsion technique. The F6 Miglitol floating microsphere was optimized formulation demonstrated with excellent drug entrapment performance (86.57%), good floating behaviour (94.25%), and the largest particle size (670µm). The present study concludes that floating based gastro retentive delivery system of Miglitol microspheres has a safe and effective drug delivery system with increased therapeutic efficacy and a longer duration of action.


2020 ◽  
Vol 10 (3) ◽  
pp. 408-417
Author(s):  
Jyotsana R. Madan ◽  
Izharahemad N. Ansari ◽  
Kamal Dua ◽  
Rajendra Awasthi

Purpose : The objective of this work was to formulate casein (CAS) nanocarriers for the dissolution enhancement of poorly water soluble drug celecoxib (CLXB). Methods: The CLXB loaded CAS nanocarriers viz., nanoparticles, reassembled CAS micelles and nanocapsules were prepared using sodium caseinate (SOD-CAS) as a carrier to enhance the solubility of CLXB. The prepared formulations were characterized for particle size, polydispersity index, zeta potential, percentage entrapment efficiency, and surface morphology for the selection of best formulation. Fourier transform infrared spectroscopy, differential scanning calorimetry and X-ray powder diffraction study was used to for the confirmation of encapsulation of CLXB. Further, in vitro drug dissolution, ex-vivo permeation studies on chicken ileum and stability studies were carried out. Results: The CLXB loaded casein nanoparticles (CNP) (batch A2) showed a particle size diameter 216.1 nm, polydispersity index 0.422 with percentage entrapment efficiency of 90.71% and zeta potential of -24.6 mV. Scanning electron microscopy of suspension confirmed globular shape of CNP. The in vitro release data of optimized batch followed non Fickian diffusion mechanism. The ex vivo permeation studies on chicken ileum of CLXB loaded CNP showed permeation through mucous membrane as compared to pure CLXB. The apparent permeability of best selected freeze dried CLXB loaded CNP (batch A2) was higher and gradually increased from 0.90 mg/cm2 after 10 min to a maximum of 1.95 mg/cm2 over the subsequent 90 min. A higher permeation was recorded at each time point than that of the pure CLXB. Conclusion: The study explored the potential of CAS as a carrier for solubility enhancement of poorly water soluble drugs.


2013 ◽  
Vol 2013 ◽  
pp. 1-10 ◽  
Author(s):  
Bhavin K. Patel ◽  
Rajesh H. Parikh ◽  
Pooja S. Aboti

Objective. The main objective of the present investigation was to develop and optimize oral sustained release Chitosan nanoparticles (CNs) of rifampicin by design of experiment (DOE). Methodology. CNs were prepared by modified emulsion ionic gelation technique. Here, inclusion of hydrophobic drug moiety in the hydrophilic matrix of polymer is applied for rifampicin delivery using CN. The 23 full-factorial design was employed by selecting the independent variables such as Chitosan concentration (X1), concentration of tripolyphosphate (X2), and homogenization speed (X3) in order to achieve desired particle size with maximum percent entrapment efficiency and drug loading. The design was validated by checkpoint analysis, and formulation was optimized using the desirability function. Results. Particle size, drug entrapment efficiency, and drug loading for the optimized batch were found to be 221.9 nm, 44.17 ± 1.98% W/W, and 42.96 ± 2.91% W/W, respectively. In vitro release data of optimized formulation showed an initial burst followed by slow sustained drug release. Kinetic drug release from CNs was best fitted to Higuchi model. Conclusion. Design of Experiment is an important tool for obtaining desired characteristics of rifampicin loaded CNs. In vitro study suggests that oral sustained release CNs might be an effective drug delivery system for tuberculosis.


2020 ◽  
Vol 15 (1) ◽  
pp. 41-67
Author(s):  
Shreya Kaul ◽  
Neha Jain ◽  
Jaya Pandey ◽  
Upendra Nagaich

Introduction: The main purpose of the research was to develop, optimize and characterize tobramycin sulphate loaded chitosan nanoparticles based gel in order to ameliorate its therapeutic efficacy, precorneal residence time, stability, targeting and to provide controlled release of the drug. Methods: Box-Behnken design was used to optimize formulation by 3-factors (chitosan, STPP and tween 80) and 3-levels. Developed formulation was subjected for characterizations such as shape and surface morphology, zeta potential, particle size, in vitro drug release studies, entrapment efficiency of drug, visual inspection, pH, viscosity, spreadability, drug content, ex vivo transcorneal permeation studies, ocular tolerance test, antimicrobial studies, isotonicity evaluation and histopathology studies. Results: Based on the evaluation parameters, the optimized formulation showed a particle size of 43.85 ± 0.86 nm and entrapment efficiency 91.56% ± 1.04, PDI 0.254. Cumulative in vitro drug release was up to 92.21% ± 1.71 for 12 hours and drug content was found between 95.36% ± 1.25 to 98.8% ± 1.34. TEM analysis unfolded spherical shape of nanoparticles. TS loaded nanoparticulate gel exhibited significantly higher transcorneal permeation as well as bioadhesion when compared with marketed formulation. Ocular tolerance was evaluated by HET-CAM test and formulation was non-irritant and well-tolerated. Histopathology studies revealed that there was no evidence of damage to the normal structure of the goat cornea. As per ICH guidelines, stability studies were conducted and were subjected for 6 months. Conclusion: Results revealed that the developed formulation could be an ideal substitute for conventional eye drops for the treatment of bacterial keratitis.


Author(s):  
Gurpreet Kandav ◽  
D.c. Bhatt ◽  
Deepak Kumar Jindal

Objective: The objective of the present investigation was to fabricate and characterize allopurinol loaded chitosan nanoparticles (A-CNPs) for sustained release of drug. Methods: The allopurinol loaded chitosan nanoparticles were successfully prepared by employing the ionotropic gelation method. Further, particle size (PS), polydispersity index (PDI), zeta potential (ZP), Differential Scanning Calorimetry (DSC), entrapment efficiency (EE), Transmission Electron Microscopy (TEM), in vitro drug release, X-Ray Diffraction (XRD) and Fourier transform infrared (FTIR) were used for evaluating formulated A-CNPs Results: A-CNPs was successfully prepared and the particle size, polydispersity index, ZP and entrapment efficiency were found to be 375.3±10.1 nm, 0.362±0.01 and 32.5±2.7 mV and 52.56±0.10% respectively. In vitro release profile of A-CNPs showed sustained release and Higuchi model was found to be best fit for drug release kinetics. FTIR study depicted no chemical interaction between pure drug allopurinol (AL) and other excipients. Conclusion: The sustained release formulation of allopurinol was successfully prepared using HMW chitosan and evaluated for different parameters.


Author(s):  
Sukhbir Kaur ◽  
Chawla V ◽  
Narang R K ◽  
Aggarwal G

Objective: The objective of this study is to compare the mucopenetration ability of metronidazole loaded chitosan (CS) and pegylated CS nanoparticles.Methods: Nanoparticles were prepared by ionic gelation technique using negatively charged pH sensitive polymer, hydroxyl propyl methyl cellulose phthalate with positively charged CS and methoxy polyethylene glycol-grafted-CS (mPEG-g-CS). mPEG-g-CS was synthesized by formaldehyde linkage method and characterized by Fourier transform infrared spectroscopy. The optimized formulations were compared for morphology, particle size, polydispersity index (PDI), entrapment efficiency, bioadhesion detachment force, in vitro and in vivo mucopenetration for CS-mPEG-g-CS nanoparticles.Results: The morphological assessment revealed smooth spherical particles with uniform dispersions. The optimized formulations particle size was found to be 202.7±27 nm and 294.1±46 nm, zeta potential 26.94±2.4 mV and 6.0±1.3 mV. PDI 0.231 and 0.268, entrapment efficiency 79.8±5.4% and 83.6±9.7%, bio-adhesion detachment force 14.98*103 dyne/cm2 and 10.67*103 dynes/cm2, in vitro mucopenetration 78% and 98% for CS-mPEG-g-CS, respectively. The qualitative in vivo mucopenetration result confirms retention of fluorescein isothiocyanate (FITC) labeled mPEG-g-CS nanoparticles till 24 hrs.Conclusion: Nanoparticles with lesser zeta potential and mucoadhesion showed higher mucosal penetration which is evident from FITC labeled histopathological mucus penetration test. Studies thus provided evidence that planned pharmaceutical strategies open new vistas for effective treatment of mucosal infections.


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