Controlled release mechanism of complex bio-polymeric emulsifiers made microspheres embedded in sodium alginate based films

Food Control ◽  
2017 ◽  
Vol 73 ◽  
pp. 1275-1284 ◽  
Author(s):  
Xi Chen ◽  
Li-xin Lu ◽  
Xiaolin Qiu ◽  
Yali Tang
Author(s):  
D. GANESH ◽  
P. SURESH ◽  
G. SRINIVAS RAO

Objective: The objective of this study is to fabricate sodium alginate (SA)/gum ghatti (GG) microbeads intercalated with Kaolin (KA) nano clay for the sustained release of curcumin (CUR). Methods: The microbeads were prepared by a simple ionotropic gelation technique. The developed beads were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), X-ray diffraction (X-RD), and scanning electron microscopy (SEM). Swelling studies and in vitro release studies were investigated under both pH 7.4 and pH 1.2 at 37 °C. Results: The developed microbeads were characterized by FTIR, which confirms the interaction between CUR, polymeric matrix and KA. DSC and XRD analysis reveals that the CUR has molecularly dispersed in the polymer matrix. In vitro results illustrated that microbeads were influenced by the pH of test media, which might be suitable for intestinal drug delivery. The drug release mechanism was analyzed by fitting the release data into different kinetic equations and n values are obtained in the range of 0.609-0.640, suggesting that the developed microbeads showed the non-Fickian diffusion type drug release. Conclusion: These results clearly illustrated that the developed KA intercalated polymeric microbeads are potential drug carriers for the controlled release of CUR.


2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Chukwuebuka H. Ozoude ◽  
Chukwuemeka P. Azubuike ◽  
Modupe O. Ologunagba ◽  
Sejoro S. Tonuewa ◽  
Cecilia I. Igwilo

Abstract Background Khaya gum is a bark exudate from Khaya senegalensis (Maliaecae) that has drug carrier potential. This study aimed to formulate and comparatively evaluate metformin-loaded microspheres using blends of khaya gum and sodium alginate. Khaya gum was extracted and subjected to preformulation studies using established protocols while three formulations (FA; FB and FC) of metformin (1% w/v)-loaded microspheres were prepared by the ionic gelation method using 5% zinc chloride solution as the cross-linker. The formulations contained 2% w/v blends of khaya gum and sodium alginate in the ratios of 2:3, 9:11, and 1:1, respectively. The microspheres were evaluated by scanning electron microscopy, Fourier transform-infrared spectroscopy, differential scanning calorimetry, entrapment efficiency, swelling index, and in vitro release studies. Results Yield of 28.48%, pH of 4.00 ± 0.05, moisture content (14.59% ± 0.50), and fair flow properties (Carr’s index 23.68 ± 1.91 and Hausner’s ratio 1.31 ± 0.03) of the khaya gum were obtained. FTIR analyses showed no significant interaction between pure metformin hydrochloride with excipients. Discrete spherical microspheres with sizes ranging from 1200 to 1420 μm were obtained. Drug entrapment efficiency of the microspheres ranged from 65.6 to 81.5%. The release of the drug from microspheres was sustained for the 9 h of the study as the cumulative release was 62% (FA), 73% (FB), and 80% (FC). The release kinetics followed Korsmeyer-Peppas model with super case-II transport mechanism. Conclusion Blends of Khaya senegalensis gum and sodium alginate are promising polymer combination for the preparation of controlled-release formulations. The blend of the khaya gum and sodium alginate produced microspheres with controlled release properties. However, the formulation containing 2:3 ratio of khaya gum and sodium alginate respectively produced microspheres with comparable controlled release profiles to the commercial brand metformin tablet.


Author(s):  
Sreeja C Nair ◽  
Karthika Ramesh ◽  
Krishnapriya M ◽  
Asha Paul

ABSTRACTObjective: The objective behind our study is that a mucoadhesive rectal hydrogel chitosan sodium alginate carbamazepine (CBZ) microspheres forthe purpose of controlled release for the treatment of epilepsy to avoid the possible side effects.Methods: The study was conducted to formulate controlled release chitosan sodium alginate CBZ microspheres with the dispersion of CBZ into thenatural polymers chitosan and sodium alginate forming microspheres conducting along with their evaluation studies.Results: The formulated microspheres were subjected to various evaluation parameters, and all the physical parameters examined are within theacceptable limits. Further, the optimized microsphere formulation (CM5) was characterized. Hence, the developed optimized microsphere formulation(CM5) seems to be a viable substitute to conventional drug delivery system for the effective management of epilepsy.Conclusion: The prepared formulation also provides a desired CBZ loaded sodium alginate microspheres with the controlled release drug delivery.Keywords: Carbamazepine, Sodium alginate microspheres, Particle size.


Author(s):  
Preethi G. B. ◽  
Prashanth Kunal

<p><strong>Objective: </strong>The current work was attempted to formulate and evaluate a controlled-release matrix-type ocular inserts containing a combination of brimonidine tartrate and timolol maleate, with a view to sustain the drug release in the cul-de-sac of the eye.<strong></strong></p><p><strong>Methods: </strong>Initially, the infrared studies were done to determine the drug–polymer interactions. Sodium alginate-loaded ocuserts were prepared by solvent casting technique. Varying the concentrations of polymer—sodium alginate, plasticizer—glycerine, and cross-linking agent—calcium chloride by keeping the drug concentration constant, made a total of nine formulations. These formulations were evaluated for its appearance, drug content, weight uniformity, thickness uniformity, percentage moisture loss, percentage moisture absorption, and <em>in vitro </em>release profile of the ocuserts. Finally, accelerated stability studies and the release kinetics were performed on the optimised formulation.<strong></strong></p><p><strong>Results: </strong>It was perceived that polymer, plasticizer, and calcium chloride had a significant influence on the drug release. The data obtained from the formulations showed that formulation—F9 was the optimised formulation, which exhibited better drug release. The release data of the optimised formulation tested on the kinetic models revealed that it exhibited first-order release kinetics. <strong></strong></p><p><strong>Conclusion: </strong>It can be concluded that a natural bioadhesive hydrophilic polymer such as sodium alginate can be used as a film former to load water soluble and hydrophilic drugs like brimonidine tartrate and timolol maleate. Among all formulations, F9 with 400 mg sodium alginate, 2% calcium chloride and 60 mg glycerin were found to be the most suitable insert in terms of appearance, ease of handling, thickness, <em>in vitro</em> drug release and stability.</p>


Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 243 ◽  
Author(s):  
Yao Yang ◽  
Zhengwei Huang ◽  
Xuan Zhang ◽  
Jinyuan Li ◽  
Ying Huang ◽  
...  

Major depressive disorder (MDD) is one of the main contributors to disability and suicide mortality globally. Paroxetine hydrochloride (PHH) is the most potent antidepressant used for MDD treatment. Due to its reduced side effects PAXIL® CR is a widely-used controlled-release formulation of PHH. However, the complicated double-layer production of PAXIL® CR faces the risk of layer separation. In this study, PHH enteric coating single layer controlled-release tablets (PHH-EC-SLTs) were designed as a simplified substitution of PAXIL® CR through a rational formulation screening. The optimized PHH-EC-SLTs showed similar release behaviors in vitro to PAXIL® CR and the release profiles corresponded to a zero-order release model (R2 = 0.9958). Polymer matrix erosion was the main release mechanism, according to the fitting exponents n > 1 in the Korsmeyer-Pappas model. Crucial pharmacokinetic parameters including peak-reaching time (Tmax), peak concentration (Cmax) and the area under the blood level-time curve (AUC0-48) of PHH-EC-SLTs and PAXIL® CR had no significant difference (p > 0.05) and the relative bioavailability (F = 97.97%) of PHH-EC-SLTs demonstrated their similar pharmacokinetic profiles in vivo. In view of avoiding layer separation risk and simplifying the preparation processing, the self-made PHH-EC-SLTs could be considered as a safe and economic alternative to PAXIL® CR.


Author(s):  
Barkat Khan ◽  
Faheem Haider ◽  
Kifayat Shah ◽  
Bushra Uzair ◽  
Kaijian Hou ◽  
...  

This study was carried out to formulate and evaluate controlled release (CR) matrix tablets of Acyclovir using combination of hydrophilic and hydrophobic polymers. Acyclovir is a guanine derivative and is its half-life is short hence administered five times a day using immediate release tablets. Six formulations (F1-F6) were developed using Ethocel and Carbopol in equal combinations at drug-polymer (D:P) ratio of 10:5, 10:6, 10:7, 10:8, 10:9 and 10:10. Solubility study was performed using six different solvents. The compatibility studies were carried out using FTIR and DSC. According to USP, Quality Control and dimensional tests (hardness, friability, disintegration and thickness) were executed. In-vitro drug release studies of Acyclovir was carried out in dissolution apparatus using using 0.1 N HCl medium at constant temperature of 37 ± 0.5 ºC. In order to analyze the drug release kinetics, five different mathematical models were applied to the release data. The results showed that there was no incompatibility between drug and polymers. Physical QC tests were found within limits of USP. The release was retarded upto 24 hrs and non-fickian in-vitro drug release mechanism was found. A formulation developed using blend of polymers, showed excellent retention and desired release profiles thus providing absolute control for 24 hrs.


Author(s):  
SAKHARE SS ◽  
SAYYAD FJ

Objective: The present investigations aim to develop mucoadhesive gastrospheres of carvedilol using sodium alginate and Ocimum basilicum seed mucilage combination blend oral use. Methods: The gastrospheres were prepared by ionotropic gelation method using 32 factorial designs, the concentration of sodium alginate and O. basilicum mucilage was independent variables while % drug content (DC), % entrapment efficiency, and % drug release at 12 h were dependent variables. The gastrospheres were evaluated for other parameters such as Fourier-transform infrared (FTIR), powder X-ray diffraction, differential scanning calorimetric, and in vitro mucoadhesion studies. Results: In optimization studies from statistical second-order complete model equation among the polymers used O. basilicum mucilage had a more profound effect on DC and % encapsulation efficiency as compared to sodium alginate. The mean particle size of gastrospheres when measured by optical microscopy technique ranged from 774 to 882 μm. The percentage of gastrosphere adhering to goat intestinal mucosal tissue varied from 10% to 65% over 8 h in 0.1N HCl, whereas this was varied from 40% to 60% in phosphate buffer pH 6.8 with provided 12 h of controlled release following zero-order release pattern. Conclusion: Studies conclude that mucilage of O. basilicum can be used as controlled release mucoadhesive material in the formulation of gastrospheres.


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