scholarly journals Preparation, Optimization, and Screening of the Effect of Processing Variables on Agar Nanospheres Loaded with Bupropion HCl by a D-Optimal Design

2015 ◽  
Vol 2015 ◽  
pp. 1-13 ◽  
Author(s):  
Jaleh Varshosaz ◽  
Mohammad Reza Zaki ◽  
Mohsen Minaiyan ◽  
Jaafar Banoozadeh
Keyword(s):  
Optimal Design ◽  
Response Surface ◽  
Calcium Chloride ◽  
Drug Loading ◽  
Antidepressant Drug ◽  
Pulmonary Delivery ◽  
Extended Period ◽  
Immediate Release ◽  
Serum Levels ◽  
High Degree

Bupropion is an atypical antidepressant drug. Fluctuating in its serum levels following oral administration of immediate release dosage forms leads to occasional seizure. The aim of the present work was designing of sustained release bupropion HCl nanospheres suited for pulmonary delivery. Agar nanospheres were prepared by transferring the w/o emulsion to solid in oil (s/o) suspension. Calcium chloride was used as cross-linking agent and hydroxypropylβ-cyclodextrin (HPβCD) was used as permeability enhancer. A response surface D-optimal design was used for optimization of nanospheres. Independent factors included in the design were calcium chloride percent, speed of homogenization, agar percent, and HPβCD percent. Optimum condition was predicted to be achieved when the calcium chloride was set at 7.19%, homogenization speed at 8500 rpm, agar content at 2%, and HPβCD at 0.12%. The optimized nanoparticles showed particle size of 587 nm, zeta potential of −30.9 mV, drug loading efficiency of 38.6%, and release efficiency of 51% until 5 h. The nanospheres showed high degree of bioadhesiveness. D-optimal response surface method is a satisfactory design to optimize the fabrication of bupropion HCl loaded agar nanospheres and these nanospheres can be successively exploited to deliver bupropion in a controlled manner for a sufficiently extended period.

scholarly journals Formulation and Mathematical Optimization of Controlled Release Calcium Alginate Micro Pellets of Frusemide

2013 ◽  
Vol 2013 ◽  
pp. 1-14 ◽  
Author(s):  
Amitava Ghosh ◽  
Prithviraj Chakraborty
Keyword(s):  
Sodium Alginate ◽  
Calcium Alginate ◽  
Mathematical Optimization ◽  
Extended Period ◽  
Cost Effective ◽  
Polynomial Equation ◽  
Chronic Hypertension ◽  
Order Polynomial ◽  
High Degree

Objective. Frusemide loaded calcium alginate micropellets, an oral microparticulate delivery system, was statistically optimized exhibiting prolonged therapeutic action minimizing its adverse effects.Methods. Ionotropic Gelation technique was adopted employing 32Factorial designs and keeping the entire process free from organic solvents. Physicochemical and the release characteristics of the prepared formulations were studied, keeping variations only in sodium alginate (primary polymer) and Acrycoat E30D (copolymer) dispersion.Result. Sodium alginate was predominant over Acrycoat E30D in all batches. Nonadditives or interaction was observed to be insignificant. Multiple regressions produced second-order polynomial equation, and the predictive results obtained were validated with high degree of correlation. Thein vivostudy applauded that optimized calcium alginate micropellets of frusemide can produce a much greater diuretic effect over an extended period of 24 hours.Conclusion. This study reveals that the potential of a single dose of the mathematically optimized micro pellets of frusemide formulation is sufficient in the management of peripheral edema and ascites in congestive heart failure and as well in the treatment of chronic hypertension, leading to better patient compliance, and can be produced with minimum experimentation and time, proving far more cost-effective formulation than the conventional methods of formulating dosage forms.

SCREENING OF BIODEGRADABLE POLYMER AND MOST EFFECTIVE VARIABLES IN PREPARATION OF ESSENTIAL OIL LOADED NANO PARTICLES FOR PULMONARY DELIVERY USING TAGUCHI DESIGN

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (02) ◽  
pp. 68-75
Author(s):  
Avani Khristi ◽  
Lalit L. Jha ◽  
Abhay Dharamsi ◽  
Keyword(s):  
Particle Size ◽  
Essential Oil ◽  
Biodegradable Polymers ◽  
Drug Loading ◽  
Pulmonary Inflammation ◽  
Pulmonary Delivery ◽  
Entrapment Efficiency ◽  
Nano Particles ◽  
Favorable Conditions ◽  
Insoluble Polymers

The biodegradability of inhalable nanoparticles (NPs) is an important criterion in prevention of lung toxicity due to NPs which have been taken to cure the condition. Pulmonary inflammation may result due to non-biodegradation or insoluble polymers used to produce NPs. Biodegradable polymers are widely used for manufacturing safe drug-entrapped inhalable NPs for pulmonary delivery. Here in this study, for preparing ajwain essential oil loaded NPs for pulmonary delivery, biodegradable polymers chitosan, gelatin and alginic acid have been evaluated for suitability. Based on the results of trial batches prepared from each polymer, the responses particle size and entrapment efficiency were measured and compared. Out of the three polymers, chitosan was having very good entrapment efficiency, poly dispersive index, drug loading and zeta potential-favorable conditions for pulmonary delivery of essential oils. Further screening of most effective variables in manufacturing nano particles using chitosan, eight batches of nano particles have been prepared as per taguchi orthogonal 2 level array L8 experimental design (Design expert software, version 7.0) where two responses, particle size and entrapment efficiency, have been observed. Based on the results of eight batches, standard effects have been calculated and significant variables identified, for both particle size and entrapment efficiency, for further optimization under design of experiment.

scholarly journals Response Surface Optimization of Bioactive Compounds Extraction from Buchholzia coriacea Using D-Optimal Design

2020 ◽  
Vol 2 (3) ◽  
pp. 175
Author(s):  
Oyedoh Eghe Amenze ◽  
Ekhorugue Uhunoma Endurance ◽  
Ijeli Ikechukwu Michael ◽  
Ayodele Bamidele Victor
Keyword(s):  
Optimal Design ◽  
Response Surface ◽  
Bioactive Compounds ◽  
Response Surface Optimization ◽  
Surface Optimization

scholarly journals Synthesis and Characterization of Stearic Acid-Beclomethasone Dipropionate Conjugates with the Potential for Improving Loading Capacity in Lipid-based Nanoparticles

2021 ◽  
Author(s):  
Shishuai Dang ◽  
Zhengwei Huang ◽  
Ying Huang ◽  
Xin Pan ◽  
Chuanbin Wu
Keyword(s):  
Drug Delivery ◽  
Stearic Acid ◽  
Beclomethasone Dipropionate ◽  
Drug Loading ◽  
Pulmonary Delivery ◽  
Dynamics Simulation ◽  
Loading Capacity ◽  
Technology Platform ◽  
New Type ◽  
Model Drug

<p>Lipid-based nanoparticles (LBNs) are a new type of nanoparticulate drug delivery system, which have been gradually shown broad prospects in pulmonary drug delivery systems. However, the main disadvantage of these LBNs for inhalable drugs with limited lipophilicity is the low encapsulation capacity. Herein, this study anticipates establishing a technology platform to improve the loading capacity of low lipophilicity drugs in LBNs, for the therapy of lung diseases. A proof-of-concept was carried out using Beclomethasone dipropionate (BDP) as a model drug. BDP was conjugated with stearic acid (SA), a kind of the lipid matrix for LBN. The conjugate was characterized and the interactions between the conjugate and SA were investigated by molecular dynamics simulation. It is expected that the drug loading capacity of weak-lipophilic drugs in LBN can be increased by establishing the technology platform, and the application of LBNs in pulmonary delivery can be broadened.</p>

scholarly journals Development of optimized formulation of liposome using 3-factor Box-Behnken Design

2021 ◽  
Vol 11 (3) ◽  
Author(s):  
Mahendra Chouhan ◽  
Rajesh Sharma ◽  
Kamlesh Dashora
Keyword(s):  
Response Surface ◽  
Polymer Coating ◽  
Drug Loading ◽  
Membrane System ◽  
Acidic Ph ◽  
Box Behnken Design ◽  
Vesicle Size ◽  
Surface Graph ◽  
Ph Dependent ◽  
Ph Sensitive Polymer

The objective of our present study is to optimize Chitosan coated liposomes formulation by Response surface methodology using 3-factor Box-Behnken Design. Different polymers based liposomes used for delivery of stable pH dependent formulation. Chitosan has been used as a pH sensitive polymer coating to target nanoparticles specifically to tumors which have a slightly acidic pH. Closed membrane system can accommodate amphiphilic or lipophilic drugs in vesicles. The optimized batch was formulated as a liposome delivery system and evaluation was done. To evaluate the unentrapped drug Shimadzu UV-Spectrometry at 228 nm was used and absorbance was noted. Response surface graph was prepared to predict value and the optimized formulation (Chitosan coated liposomes) can be used for loading of bio-active.The values of percent drug entrapment and average vesicle size were presented and found formulation F3&F5 were optimized for further evaluating on basis of particle size and drug loading.

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