Physicochemical characterization of asulacrine towards the development of an anticancer liposomal formulation via active drug loading: Stability, solubility, lipophilicity and ionization

2014 ◽  
Vol 473 (1-2) ◽  
pp. 528-535 ◽  
Author(s):  
Esther See ◽  
Wenli Zhang ◽  
Jianping Liu ◽  
Darren Svirskis ◽  
Bruce C. Baguley ◽  
...  
Author(s):  
A. Hasrawati ◽  
Irsan Rizaldi ◽  
Deisy Febrianti ◽  
A Mumtihanah Mursyid ◽  
Neneng Amelia Bakri

Objective: Thymoquinone is a main component of Black Cumin (Nigella  sativa Linn.) with various pharmacological activities, but has poor stability and bioavailability. The purpose of this study was to carry out the preparation and characterization of timoquinone nanoparticles PEGylation. Methods: The Thymoquinone nanoparticles  (TQ-NP) were made with PEGylation using PEG 6000 with the concentrations on each preparation of 3 mM (A), 4 mM (B), and 5 mM (C) then were evaluated by the parameter of yield percentage Entrapment Efficiency (EE) and Drug Loading (DL), drug release, size and distribution particle, morphological analysis and Fourier Transform-Infrared spectrophotometer (FTIR). Results: Thymoquinone nanoparticle was PEGylated with PEG 6000  has the highest efficiency entrapment of 99.9718±0.029% in formula A, with the capacity of drug loading 0,66%. Formulation A release 99.9718±0.029% of Thymoquinone at 50 minutes. The morphological observations with Scanning Electron Microscope (SEM) showed spherical nanoparticles morphology.                           Peer Review History: Received 11 September  2020; Revised 5 Decembe; Accepted 3 January, Available online 15 January 2021 UJPR follows the most transparent and toughest ‘Advanced OPEN peer review’ system. The identity of the authors and, reviewers will be known to each other. This transparent process will help to eradicate any possible malicious/purposeful interference by any person (publishing staff, reviewer, editor, author, etc) during peer review. As a result of this unique system, all reviewers will get their due recognition and respect, once their names are published in the papers. We expect that, by publishing peer review reports with published papers, will be helpful to many authors for drafting their article according to the specifications. Auhors will remove any error of their article and they will improve their article(s) according to the previous reports displayed with published article(s). The main purpose of it is ‘to improve the quality of a candidate manuscript’. Our reviewers check the ‘strength and weakness of a manuscript honestly’. There will increase in the perfection, and transparency. Received file:                           Comments of reviewer(s):         Average Peer review marks at initial stage: 6.0/10 Average Peer review marks at publication stage: 8.0/10 Reviewer(s) detail: Dr. Evren Alğin Yapar, Turkish Medicines and Medical Devices Agency, Turkiye, [email protected] Dr. Sally A. El-Zahaby, Pharos University in Alexandria, Egypt, [email protected] Similar Articles: ABACAVIR LOADED NANOPARTICLES: PREPARATION, PHYSICOCHEMICAL CHARACTERIZATION AND IN VITRO EVALUATION LONG CHAIN POLYMERIC CARBOHYDRATE DEPENDENT NANOCOMPOSITES IN TISSUE ENGINEERING EFFECT OF PEGYLATED EDGE ACTIVATOR ON SPAN 60 BASED- NANOVESICLES: COMPARISON BETWEEN MYRJ 52 AND MYRJ 59


2003 ◽  
Vol 14 (5) ◽  
pp. 899-908 ◽  
Author(s):  
Paolo Caliceti ◽  
Stefano Salmaso ◽  
Alessandra Semenzato ◽  
Tommaso Carofiglio ◽  
Roberto Fornasier ◽  
...  

Author(s):  
ARIF BUDIMAN

Solubility of the drug has a strong influence to achieve higher bioavailability of the drug in systemic circulation. More than 70% NCEs (new chemical entities) are hydrophobic, and practically difficult into solid formulation due to their poor water solubility. Mesoporous silicas (MSP) have been used for drug delivery system, especially for poorly water-soluble drugs. Encapsulation and interaction of drugs in MSP can enhance the delivery and maintain the stability of the drug. However, the characterization of the drug in MSP is necessary to confirm its molecular state. In this review, we present an overview of reports related to the characterization of drug encapsulated into MSP. Encapsulation of drugs in MSP can prevent recrystallization of drugs due to its inhibition of crystal nucleation. A porous material in MSP can maintain the drug in a physically stable amorphous state. The preventing of drug crystallization in MSP can enhance the solubility and the dissolution rate of drug. Therefore, in this work, attempts have been made to understand the molecular state of the drug in MSP. The physicochemical characterization of drug by transmission electron microscopy (TEM), scanning electron microscope (SEM), differential scanning calorimetry (DSC), fourier-transform infrared spectroscopy (FTIR), powder x-ray diffraction (PXRD) and thermogravimetric analysis (TGA) were discussed. The effect of solvent and methods of drug loading and the effect of the shape of MSP on release profiles are also presented. Overall, this review provides information about the characterization of drug encapsulated into MSP which will be useful in pharmaceutical formulation development.


2019 ◽  
Vol 38 (2) ◽  
pp. 385 ◽  
Author(s):  
Marwa M. El-Naggar ◽  
Wael S. I. Abou-Elmagd ◽  
Ashraf Suloma ◽  
Hamza A. El-Shabaka ◽  
Magdy T. Khalil ◽  
...  

Author(s):  
Kumar P ◽  
S Kumar ◽  
A Kumar ◽  
M Chander

The purpose of this study was to prepare and characterize solid dispersions of the antibacterial agent Cefdinir with PEG 4000 and PVP K-30 with a view to improve its dissolution properties. Investigations of the properties of the dispersions were performed using release studies, X-ray powder diffraction (XRD) and Fourier transform infrared (FTIR). The results obtained showed that the rate of dissolution of Cefdinir was considerably improved when formulated in solid dispersions with PVP K-30 and PEG 4000 as compared with pure drug and physical mixtures. The results from XRD studies showed the transition of crystalline nature of drug to amorphous form, while FTIR studies demonstrated the absence of drug-carriers interaction.


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