scholarly journals Cefdinir Inclusion in Mesoporous Silica as Effective Dissolution Enhancer with Improved Physical Stability

2021 ◽  
Vol 11 ◽  
pp. 73-86
Author(s):  
Raghad Al Nuss ◽  
Hind El Zein
Keyword(s):  
Drug Release ◽  
Mesoporous Silica ◽  
Release Kinetics ◽  
Physical Stability ◽  
Amorphous State ◽  
Weibull Model ◽  
Drug Dissolution ◽  
Scanning Calorimetry ◽  
Immersion Method ◽  
Amorphous Form

Objective: The objective of this research was to enhance the physical stability and the dissolution rate of cefdinir, a BCS class IV drug, characterized by low and variable bioavailability due to both its low solubility and low permeability. Methods: Cefdinir was loaded into the mesoporous silica (SBA-15), by using the solvent immersion method starting from different organic solvents. And then formula (F3), which exhibited the highest loading percentage, was selected to study its drug release in media with different pH (1.2, 4.5, and 6.8), and has been fully characterized by using: Fourier Transform Infrared Spectroscopy (FT-IR) Spectroscopy, Differential Scanning Calorimetry, Powder X-ray Diffraction, and has been subjected to accelerated stability tests using different temperatures and relative humidity. Drug release kinetics were studied by using the following models: Probit, Gompertz, Weibull, and Logistic. Results: The results showed a remarkable dissolution improvement of cefdinir from the loaded silica in comparison to the crystalline drug at the different studied media. Drug release behaviors were well simulated by the Weibull model for F3 in all studied media and for pure Cefdinir in phosphate buffer only, and by the Gompertz function for pure Cefdinir in HCl buffer and Acetate buffer. FTIR results showed hydrogen bonds formed between the drug and silica, DSC and PXRD results revealed the transformation of cefdinir into an amorphous form upon adsorption. Stability studies under different conditions revealed the ability of mesoporous silica to maintain the amorphous state of the drug, which has been formed upon adsorption, and to prevent re-organization in the crystal nucleus of the drug molecules. Conclusion: Thus, loading cefdinir onto mesoporous silica can be used as a promising method to enhance drug dissolution, and maintain the physical stability of its amorphous form.

Mesoporous Silica Molecular Sieve based Nanocarriers: Transpiring Drug Dissolution Research

2017 ◽  
Vol 23 (3) ◽  
pp. 467-480 ◽  
Author(s):  
Satyanarayan Pattnaik ◽  
Kamla Pathak
Keyword(s):  
Drug Release ◽  
Mesoporous Silica ◽  
Molecular Sieves ◽  
Release Kinetics ◽  
Drug Loading ◽  
Scale Up ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Water Soluble Drugs ◽  
Loading Methods

Background: Improvement of oral bioavailability through enhancement of dissolution for poorly soluble drugs has been a very promising approach. Recently, mesoporous silica based molecular sieves have demonstrated excellent properties to enhance the dissolution velocity of poorly water-soluble drugs. Description: Current research in this area is focused on investigating the factors influencing the drug release from these carriers, the kinetics of drug release and manufacturing approaches to scale-up production for commercial manufacture. Conclusion: This comprehensive review provides an overview of different methods adopted for synthesis of mesoporous materials, influence of processing factors on properties of these materials and drug loading methods. The drug release kinetics from mesoporous silica systems, the manufacturability and stability of these formulations are reviewed. Finally, the safety and biocompatibility issues related to these silica based materials are discussed.

scholarly journals Development of a Hydrophobicity-Controlled Delivery System Containing Levodopa Methyl Ester Hydrochloride Loaded into a Mesoporous Silica

Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 1039
Author(s):  
Tamás Kiss ◽  
Gábor Katona ◽  
László Mérai ◽  
László Janovák ◽  
Ágota Deák ◽  
...  
Keyword(s):  
Methyl Ester ◽  
Drug Release ◽  
Mesoporous Silica ◽  
Surface Area ◽  
Release Rate ◽  
Release Kinetics ◽  
Amorphous State ◽  
Ester Hydrochloride ◽  
Methyl Ester Hydrochloride ◽  
Levodopa Methyl Ester

Background: The drug release of antiparkinsonian drugs is an important issue during the formulation process because proper release kinetics can help to reduce the off periods of Parkinson’s disease. A 2-factor, 3-level (32) full-factorial design was conducted to evaluate statistically the influence of the hydrophobicity of mesoporous silica on drug release. Methods: Hydrophobization was evaluated by different methods, such as contact angle measurement, infrared spectroscopy and charge titration. After loading the drug (levodopa methyl ester hydrochloride, melevodopa hydrochloride, LDME) into the mesopores, drug content, particle size, specific surface area and homogeneity of the products were also analyzed. The amorphous state of LDME was verified by X-ray diffractometry and differential scanning calorimetry. Results: Drug release was characterized by a model-independent method using the so-called initial release rate parameter, as detailed in the article. The adaptability of this method was verified; the model fitted closely to the actual release results according to the similarity factor, independently of the release kinetics. Conclusions: The API was successfully loaded into the silica, resulting in a reduced surface area. The release studies indicated that the release rate significantly decreased (p < 0.05) with increasing hydrophobicity. The products with controlled release can reduce the off period frequency.

scholarly journals Formulation and Evaluation of Gliclazide Solid Dispersions Incorporated Tablets for Controlled Drug Release

2020 ◽  
pp. 621-629
Author(s):  
Ramisetty Sunitha ◽  
Kothakota Venugopal ◽  
Suggala Venkata Satyanarayana
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Solid Dispersion ◽  
Release Kinetics ◽  
Maximum Yield ◽  
Amorphous State ◽  
Tablet Formulation ◽  
Drug Dissolution ◽  
Fickian Diffusion ◽  
Drug Content

The current study deals with formulation and evaluation of gliclazide solid dispersion with HP β Cyclodextrin to enhance solubility and incorporate into tablet formulation for controlled release of gliclazide. Gliclazide solid dispersion (SD) prepared using varying ratios of HP β Cyclodextrin and evaluated. The optimized SD formulation incorporated into tablet by using hydroxypropyl cellulose, HPMC K 100M. The drug dissolution from tablet formulation analyzed and characterize. The formulation SD3 comprising of drug and polymer in 1:3 ratio displayed 43-fold increase in solubility when compared to pure drug. The formulation SD13 displayed maximum yield of 98.96% and maximum drug content of 99% chosen optimal for tablet formulation. FTIR studies revealed that there is no incompatibility between drug and polymers found. XRD studies revealed that the optimized solid dispersion formulation was found to be in amorphous state. Around 15 formulations of controlled release tablet blends evaluated for micrometric properties show that all the formulations posses’ good flow properties. Formulation F15 with maximum drug content of 99.99% and drug release of 99.96 % over 16h was chosen optimal and characterized. The release kinetics suggest that drug release followed zero order and release from tablets was anomalous non- fickian diffusion super case II transport. The results show that combination of solid dispersion and application of hydrophilic and hydrophobic polymers in matrix formation can facilitate better dissolution and absorption profile with greater patient compliance.

STUDIES ON UREA CO-INCLUSION COMPLEXES OF EBASTINE FOR STEEP IMPROVEMENT IN DISSOLUTION PROFILE

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (08) ◽  
pp. 35-45
Author(s):  
M. Dhall ◽  
◽  
A. K. Madan
Keyword(s):  
Dissolution Rate ◽  
Release Kinetics ◽  
Thermal Studies ◽  
Physical Stability ◽  
Molar Fraction ◽  
Aqueous Solubility ◽  
Weibull Model ◽  
Complexing Agent ◽  
Content Uniformity ◽  
Dissolution Profile

Urea co-inclusion technique has been successfully utilized for steep enhancement in dissolution rate of ebastine (EB), a BCS class II potent drug. EB is a novel second generation H1 receptor antagonist used for prevention of chronic idiopathic urticaria and allergic rhinitis. It exhibits low aqueous solubility and consequent poor bioavailability. In the present study, EB was engulfed in urea channel/tunnels along with rapidly complexing agent (RCA). Resulting complexes of EB (EBUCIC) were characterized by DSC, FTIR, XRD and 1H-NMR. Minimum proportion of RCA for incorporation of EB in hexagonal urea was determined calorimetrically. The thermal studies indicated increase in heat of decomposition with increasing molar fraction of RCA in EBUCICs, ensuring better physical stability of complexes. Content uniformity study depicted uniform composition formulation of EB. Weibull model described release kinetics of EB. Enhancement in dissolution rate ensures urea co-inclusion to be a useful approach for development of rapid/instantaneous release dosage forms.

Fabrication and characterization of smart karaya gum/sodium alginate semi-IPN microbeads for controlled release of D-penicillamine drug

2020 ◽  
pp. 096739112090447
Author(s):  
O Sreekanth Reddy ◽  
MCS Subha ◽  
T Jithendra ◽  
C Madhavi ◽  
K Chowdoji Rao
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Release Kinetics ◽  
Polymerization Reaction ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Drug Release Kinetics ◽  
Swelling Capacity ◽  
Release Data ◽  
Karaya Gum

This article reports the fabrication of pH-sensitive microbeads from sodium alginate (SA) and modified karaya gum (KG). KG was modified by graft copolymerization using 2-hydroxyethyl methacrylate (2-HEMA) through in situ free radical polymerization reaction. The graft copolymer was blended with SA to develop microbeads by a simple ionotropic gelation technique. The microbeads were characterized by Fourier transform infrared spectroscopy, X-ray diffraction, differential scanning calorimetry, thermogravimetric analysis, and scanning electron microscopy. The effect of %HEMA and polymer blend ratio on the swelling capacity was investigated. Drug release kinetics of the microbeads was investigated under both pH 7.4 and pH 1.2 at 37°C. The drug release kinetics was analyzed by evaluating the release data using different kinetic models.

Development of Diclofenac Sodium Releasing Bio-Erodible Polymeric Nanomats

2006 ◽  
Vol 6 (9) ◽  
pp. 3310-3320 ◽  
Author(s):  
A. M. Piras ◽  
L. Nikkola ◽  
F. Chiellini ◽  
N. Ashammakhi ◽  
E. Chiellini
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Release Kinetics ◽  
Diclofenac Sodium ◽  
High Surface ◽  
Active Agent ◽  
Volume Ratio ◽  
Homogeneous Distribution ◽  
Scanning Calorimetry ◽  
Nano Structure

Application of nanofiber-based nanomats in medicine is attractive and thanks to the 3D nano-structure and the high surface to volume ratio they are excellent for local controlled drug delivery. The use of bioactive bioerodible polymers for developing drug delivery nanomats may allow for drug release and targeting control. Objective of the current study was to evaluate the suitability of bioerodible polymeric material based on n-butyl hemiester of [poly(maleic anhydride-alt-2-methoxyethyl vinyl ether)] (PAM14) for the preparation of nanomats for controlled administration of anti-inflammatory, diclofenac sodium (DS) drug. Samples were prepared using different polymer concentrations (5–10%) in either ethanol or acetic acid as solvent. Morphology was investigated by using scanning electron microscopy (SEM). Thermal analysis such as differential scanning calorimetry (DSC) was performed to detect effect on polymer arrangement. DS localization in electrospun nanomats was evaluated by using electron back scattering microanalysis, based on the detection of chlorine, and drug release kinetics was assessed using UV-Vis. Average fiber diameter resulted in the range of 100 nm to 1.0 μm and a homogeneous distribution of the loaded drug into the fibers was observed. The DS release was immediate and despite the preliminary nature of the performed electrospinning experiments, the achieved results appear promising for the future development of a novel system for the controlled and targeted administration of drug and active agent.

scholarly journals Combined Self-Nanoemulsifying and Solid Dispersion Systems Showed Enhanced Cinnarizine Release in Hypochlorhydria/Achlorhydria Dissolution Model

Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 627
Author(s):  
Ahmad A. Shahba ◽  
Ahmad Y. Tashish ◽  
Fars K. Alanazi ◽  
Mohsin Kazi
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Negative Impact ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Dissolution Model ◽  
Dissolution Efficiency ◽  
Drug Free

The study aims to design a novel combination of drug-free solid self-nanoemulsifying drug delivery systems (S-SNEDDS) + solid dispersion (SD) to enhance cinnarizine (CN) dissolution at high pH environment caused by hypochlorhydria/achlorhydria. Drug-loaded and drug-free liquid SNEDDS were solidified using Neusilin® US2 at 1:1 and 1:2 ratios. Various CN-SDs were prepared using freeze drying and microwave technologies. The developed SDs were characterized by differential scanning calorimetry (DSC) and X-ray powder diffraction (XRD). In-vitro dissolution studies were conducted to evaluate CN formulations at pH 6.8. Drug-free S-SNEDDSs showed acceptable self-emulsification and powder flow properties. DSC and XRD showed that CN was successfully amorphized into SDs. The combination of drug-free S-SNEDDS + pure CN showed negligible drug dissolution due to poor CN migration into the formed nanoemulsion droplets. CN-SDs and drug-loaded S-SNEDDS showed only 4% and 23% dissolution efficiency (DE) while (drug-free S-SNEDDS + FD-SD) combination showed 880% and 160% enhancement of total drug release compared to uncombined SD and drug-loaded S-SNEDDS, respectively. (Drug-free S-SNEDDS + SD) combination offer a potential approach to overcome the negative impact of hypochlorhydria/achlorhydria on drug absorption by enhancing dissolution at elevated pH environments. In addition, the systems minimize the adverse effect of adsorbent on drug release.

Sign in / Sign up

Export Citation Format

Share Document