Controlled release evaluation of paracetamol loaded amine functionalized mesoporous silica KCC1 compared to microcrystalline cellulose based tablets

AbstractIn the pharmaceutical manufacturing, drug release behavior development is remained as one of the main challenges to improve the drug effectiveness. Recently, more focus has been done on using mesoporous silica materials as drug carriers for prolonged and superior control of drug release in human body. In this study, release behavior of paracetamol is developed using drug-loaded KCC-1-NH2 mesoporous silica, based on direct compaction method for preparation of tablets. The purpose of this study is to investigate the utilizing of pure KCC-1 mesoporous silica (KCC-1) and amino functionalized KCC-1 (KCC-1-NH2) as drug carriers in oral solid dosage formulations compared to common excipient, microcrystalline cellulose (MCC), to improve the control of drug release rate by manipulating surface chemistry of the carrier. Different formulations of KCC-1 and KCC-NH2 are designed to investigate the effect of functionalized mesoporous silica as carrier on drug controlled-release rate. The results displayed the remarkable effect of KCC-1-NH2 on drug controlled-release in comparison with the formulation containing pure KCC-1 and formulation including MCC as reference materials. The pure KCC-1 and KCC-1-NH2 are characterized using different evaluation methods such as FTIR, SEM, TEM and N2 adsorption analysis.

Download Full-text

Preparation and Drug Release Behavior of Nifedipine-Loaded Poly(lactic acid)/Polyethylene Glycol Microcapsules

Journal of Nanoscience and Nanotechnology ◽

10.1166/jnn.2021.19168 ◽

2021 ◽

Vol 21 (7) ◽

pp. 3735-3741

Author(s):

Heeseok Jeong ◽

Hyunju Lim ◽

Deuk Yong Lee ◽

Yo-Seung Song ◽

Bae-Yeon Kim

Keyword(s):

Lactic Acid ◽

Polyethylene Glycol ◽

Drug Release ◽

Release Rate ◽

Drug Carriers ◽

Poly Lactic Acid ◽

Release Behavior ◽

Drug Release Rate ◽

Water Emulsion ◽

Drug Release Behavior

Nifedipine (NF)-loaded poly(lactic acid) (PLA) and PLA/polyethylene glycol (PLA/PEG) microcapsules are synthesized using a high-speed agitator and a syringe pump with an oil-in-water emulsion-solvent evaporation technique to evaluate the effect of PLA/PEG ratio on morphology and drug release behavior of the capsules. Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimeter (DSC), and X-ray diffraction (XRD) results indicate that PEG reacts successfully with PLA due to the ether bond between PEG and PLA. The drug release rate of PLA and PLA/PEG capsules increases dramatically from 0 to 5 min and then reaches a plateau within 15 to 20 min. Due to the high specific surface area, the amount of NF released is raised by reducing the PLA concentration from 5 wt% to 2 wt%. Unlike PLA capsules, the drug release rate of PLA/PEG capsules increases due to the size effect by varying the PLA/PEG ratio from 10/0 to 6/4. Larger PLA/PEG capsules are attributed to higher amounts of encapsulated NF. The capsules show no evidence of cytotoxicity, suggesting that the PLA and PLA/PEG drug carriers are clinically safe.

Download Full-text

Formulation Development and Characterization of controlled release core in cup matrix tablets of venlafaxine HCl

Current Drug Therapy ◽

10.2174/1574885515666200331104440 ◽

2020 ◽

Vol 15 ◽

Author(s):

Balaji Maddiboyina ◽

Vikas Jhawat ◽

Gandhi Sivaraman ◽

Om Prakash Sunnapu ◽

Ramya Krishna Nakkala ◽

...

Keyword(s):

Controlled Release ◽

Drug Release ◽

Release Rate ◽

Zero Order ◽

Water Soluble ◽

Matrix Tablets ◽

Drug Dissolution ◽

Crystalline Cellulose ◽

Hydrophobic Polymers

Background: Venlafaxine HCl is a selective serotonin reuptake inhibitor which is given in the treatment of depression. The delivery of the drug at a controlled rate can be of great importance for prolonged effect. Objective: The objective was to prepare and optimize the controlled release core in cup matrix tablet of venlafaxine HCl using the combination of hydrophilic and hydrophobic polymers to prolong the effect with rate controlled drug release. Methods: The controlled release core in cup matrix tablets of venlafaxine HCl were prepared using HPMC K5, K4, K15, HCO, IPA, aerosol, magnesium sterate, hydrogenated castor oil and micro crystalline cellulose PVOK-900 using wet granulation technique. Total ten formulations with varying concentrations of polymers were prepared and evaluated for different physicochemical parameters such FTIR analysis for drug identification, In-vitro drug dissolution study was performed to evaluate the amount of drug release in 24 hrs, drug release kinetics study was performed to fit the data in zero order, first order, Hixson–crowell and Higuchi equation to determine the mechanism of drug release and stability studies for 3 months as observed. Results: The results of hardness, thickness, weight variation, friability and drug content study were in acceptable range for all formulations. Based on the In vitro dissolution profile, formulation F-9 was considered to be the optimized extending the release of 98.32% of drug up to 24 hrs. The data fitting study showed that the optimized formulation followed the zero order release rate kinetics and also compared with innovator product (flavix XR) showed better drug release profile. Conclusion: The core-in-cup technology has a potential to control the release rate of freely water soluble drugs for single administration per day by optimization with combined use of hydrophilic and hydrophobic polymers.

Download Full-text

Pectin-Chitosan Multilayer Coated Microbeads of Diclofenac Sodium Prepared by Layer-by-Layer Technique

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.1060.45 ◽

2014 ◽

Vol 1060 ◽

pp. 45-49

Author(s):

Kamonrak Cheewatanakornkool ◽

Pornsak Sriamornsak

Keyword(s):

Controlled Release ◽

Drug Release ◽

Diclofenac Sodium ◽

Gastric Fluid ◽

Layer By Layer ◽

Release Behavior ◽

Freeze Dried ◽

Layer Technique ◽

Calcium Pectinate ◽

Layer By Layer Technique

The main objective of this study was to fabricate biopolymer-based microbeads, providing enteric properties and controlled release of diclofenac sodium, using layer-by-layer technique. The calcium pectinate microbeads have been designed and coated with chitosan and pectin multilayers. Drug release was performed in simulate gastric fluid (pH 1.2) for 2 hours, followed by pH 6.8 buffer for 8 hours. The effects of chitosan concentration, number of layer and drying technique on drug release were investigated. The results showed that the calcium pectinate microbeads could be simply prepared by ionotropic gelation and then coated with chitosan and pectin solutions using layer-by-layer procedure. The diameter of the microbeads ranged from 800 to 1000 μm for air-dried samples and from 1 to 2 mm for freeze-dried samples. The freeze-dried microbeads had a rough surface and many pores inside, as observed by SEM. The microbeads coated with 4% chitosan/4% pectin revealed a slower drug release than those coated with 1% chitosan/4% pectin and demonstrated a controlled release pattern. Moreover, different drying techniques and numbers of layer also influenced drug release behavior of the prepared microbeads.

Download Full-text

Microorganism-based monodisperse microcapsules: encapsulation of the fungicide tebuconazole and its controlled release properties

RSC Advances ◽

10.1039/c5ra01629k ◽

2015 ◽

Vol 5 (32) ◽

pp. 25164-25170 ◽

Cited By ~ 6

Author(s):

Bo Zhang ◽

Teng Zhang ◽

Quanxi Wang ◽

Tianrui Ren

Keyword(s):

Controlled Release ◽

Powdery Mildew ◽

Drug Release ◽

Release Rate ◽

Drug Release Rate ◽

Burst Effect ◽

Initial Burst ◽

Release System ◽

Controlled Release System ◽

Monodisperse Microcapsules

A controlled release system was prepared, it based on UF modified PCC cells in which TEB are loaded into cells. It can control the drug release rate, depress the initial “burst effect”, and was efficacious in controlling wheat powdery mildew.

Download Full-text

Influence of functionalized mesoporous silica in controlling azathioprine drug release and cytotoxicity properties

Materials Research Innovations ◽

10.1080/14328917.2016.1265257 ◽

2017 ◽

Vol 21 (7) ◽

pp. 413-425 ◽

Cited By ~ 2

Author(s):

Suman Jangra ◽

Surender Duhan ◽

Manjeet Singh Goyat ◽

Vinod Chhokar ◽

Sandeep Singh ◽

...

Keyword(s):

Drug Release ◽

Mesoporous Silica ◽

Functionalized Mesoporous Silica

Download Full-text

A Microporous Chitosan/Collagen Composite Encapsulated Small Tube of Nanoporous Anodic Aluminum Oxide for Long-Acting Drug Release

Volume 10: Micro- and Nano-Systems Engineering and Packaging ◽

10.1115/imece2015-50949 ◽

2015 ◽

Author(s):

Bao-Ying Lee ◽

Ching-Wen Li ◽

Gou-Jen Wang

Keyword(s):

Drug Release ◽

Aluminum Oxide ◽

Release Rate ◽

Anodic Aluminum Oxide ◽

Drug Carriers ◽

Anodic Aluminum ◽

Release Device ◽

Nanoporous Anodic Aluminum Oxide ◽

Long Acting ◽

Nanoporous Anodic Aluminum

This study aims to develop a long-acting and implantable drug release device that can well control the release rate and concentration of the loaded drug. The proposed long-acting and implantable drug release device consists of a tubular nanoporous anodic aluminum oxide (AAO) and the microporous chitosan/collagen composite encapsulated inside it. The nanopore size of the AAO tube can be arranged by the anodization parameters to adjust the release rate and concentration, while the microporous chitosan/collagen composite can provide the device with a long-acting release property. Fabrication results indicated that the AAO tube has a uniform pore arrangement with pore size around 50 nm. And the synthesized microporous chitosan/collagen composites composites containing 90% of chitosan had the highest moisture content; therefore were used as the drug carriers. Release experiments demonstrate that the proposed long-acting drug release device had released only less than 60% of the loading drug at the 16th release day.

Download Full-text

Mesoporous silica nanobeans dual-functionalized with AIEgens and leaning pillar[6]arene-based supramolecular switches for imaging and stimuli-responsive drug release

Chemical Communications ◽

10.1039/c9cc07115f ◽

2019 ◽

Vol 55 (94) ◽

pp. 14099-14102 ◽

Cited By ~ 12

Author(s):

Xiangshuai Li ◽

Junyou Han ◽

Jianchun Qin ◽

Ming Sun ◽

Jiarui Wu ◽

...

Keyword(s):

Drug Release ◽

Mesoporous Silica ◽

Stimuli Responsive ◽

Tumor Inhibition ◽

Turn On ◽

Functionalized Mesoporous Silica

Dual-functionalized mesoporous silica nanobeans capable of GSH-dependent turn-on fluorescence and stimuli-responsive drug release are prepared for tumor inhibition and imaging.

Download Full-text

Eccentric magnetic microcapsules for orientation-specific and dual stimuli-responsive drug release

Journal of Materials Chemistry B ◽

10.1039/c5tb00263j ◽

2015 ◽

Vol 3 (22) ◽

pp. 4530-4538 ◽

Cited By ~ 20

Author(s):

Jingxian Huang ◽

Chongdai Luo ◽

Wanbo Li ◽

Yan Li ◽

Yu Shrike Zhang ◽

...

Keyword(s):

Drug Delivery ◽

Controlled Release ◽

Drug Release ◽

Release Behavior ◽

Stimuli Responsive

Uniform eccentric magnetic microcapsules show controlled-release behavior for orientation-specific and dual stimuli-responsive drug delivery under ultrasound and laser regulation.

Download Full-text

STUDY OF THE DIFFERENT RELEASE CHARACTERISTICS OF ANTIBIOTICS FROM PATIENTS: A DYNAMIC ELUTING SYSTEM TO INVESTIGATE DRUG RELEASE FROM ANTIBIOTIC-IMPREGNATED CALCIUM SULFATE DELIVERY

Journal of Mechanics in Medicine and Biology ◽

10.1142/s0219519415500128 ◽

2015 ◽

Vol 15 (01) ◽

pp. 1550012

Author(s):

YANG ZHANG ◽

RENJIE WU ◽

YING HU ◽

YU DONG ◽

LIFENG SHEN ◽

...

Keyword(s):

Drug Release ◽

Delivery System ◽

Release Rate ◽

Calcium Sulfate ◽

Fickian Diffusion ◽

Release Behavior ◽

Cumulative Release ◽

In Vivo Release

Background: Antibiotic-impregnated calcium sulfate delivery systems (ACDS) are commonly used to treat chronic osteomyelitis. Our research is to investigate drug release in vitro over a longer period, as a cautious predictor of in vivo release. Methods: The local release behavior of antibiotic in vitro was simulated. The consecutive dynamic eluting experiment was performed based on the pro-operative characteristic of osteomyelitis patients and the determined results of drug concentration in the human drainage tissue fluid (DTF). The concentration of each drug in the receiving solution was detected by ultra-performance liquid chromatography-tandem quadrupole detector mass spectrometry. The ACDS was reviewed by scanning electronic microscopy (SEM) after 48 h, and prepared to be eluted for another examination after 33 days. The mechanism of antibiotic release was analyzed by using the Ritger–Peppas and Weibull equations. Results: The cumulative release rate of vancomycin in a vancomycin-calcium sulfate delivery system (VCDS) was 77.50 % (3.0 mm diameter) and 72.43 % (4.8 mm diameter), while that of the tobramycin in a tobramycin-calcium sulfate delivery system (TCDS) was 88.0 % (3.0 mm diameter) and 84.55 % (4.8 mm diameter). At the 15th day, approximately 27.92% of vancomycin was and 29.35% of tobramycin was released from the local implant in vivo. Using SEM, numerous vancomycin and tobramycin particles were found to be attached to the columnar calcium sulfate crystals at the start of the experiment. The release behavior of the two antibiotics followed a combination of Fickian diffusion and Case II transport mechanisms within the first 48 h, and a Fickian diffusion mechanism during the subsequent time period. The correlation coefficient of tobramycin and vancomycin in vivo and in vitro was 0.9704–0.9949 and 0.9549–0.9782, respectively. Conclusion: A good correlation of the in vivo and in vitro cumulative release rates was observed by comparing the cumulative release rate of drugs in vitro by means of the dynamic eluting model, and in the DTF. Therefore, our study has proved that it is possible to use the dynamic eluting model as a cautious predictor of in vivo release.

Download Full-text