scholarly journals Orodispersible Membranes from a Modified Coaxial Electrospinning for Fast Dissolution of Diclofenac Sodium

Membranes ◽  
2021 ◽  
Vol 11 (11) ◽  
pp. 802
Author(s):  
Tingbao Ning ◽  
Yangjian Zhou ◽  
Haixia Xu ◽  
Shiri Guo ◽  
Ke Wang ◽  
...  
Keyword(s):  
Diclofenac Sodium ◽  
Amorphous State ◽  
Electrospun Nanofibers ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Working Fluid ◽  
Coaxial Electrospinning ◽  
Poorly Water Soluble ◽  
Fast Dissolution

The dissolution of poorly water-soluble drugs has been a longstanding and important issue in pharmaceutics during the past several decades. Nanotechnologies and their products have been broadly investigated for providing novel strategies for resolving this problem. In the present study, a new orodispersible membrane (OM) comprising electrospun nanofibers is developed for the fast dissolution of diclofenac sodium (DS). A modified coaxial electrospinning was implemented for the preparation of membranes, during which an unspinnable solution of sucralose was explored as the sheath working fluid for smoothing the working processes and also adjusting the taste of membranes. SEM and TEM images demonstrated that the OMs were composed of linear nanofibers with core-sheath inner structures. XRD and ATR-FTIR results suggested that DS presented in the OMs in an amorphous state due to the fine compatibility between DS and PVP. In vitro dissolution measurements and simulated artificial tongue experiments verified that the OMs were able to release the loaded DS in a pulsatile manner. The present protocols pave the way for the fast dissolution and fast action of a series of poorly water-soluble active ingredients that are suitable for oral administration.

BEHAVIOURAL STUDY OF CYCLODEXTRIN INCLUSION COMPLEX ON ENHANCEMENT OF SOLUBILITY OF ACECLOFENAC

INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (11) ◽  
pp. 19-23
Author(s):  
J Shaikh ◽  
◽  
S. V. Deshmane ◽  
R. N Purohit ◽  
K. R. Biyani
Keyword(s):  
Inclusion Complex ◽  
Solid Dispersion ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Phase Solubility ◽  
Solubility Study ◽  
Cyclodextrin Inclusion ◽  
Poorly Water Soluble ◽  
Cyclodextrin Inclusion Complex

The main objective of the present study was to enhance the solubility and dissolution rate of poorly water soluble aceclofenac using its solid dispersion with β-cyclodextrin. FTIR and DSC study was carried out to find out any incompatibility. The phase solubility of drug was carried out in 1, 2, 5, and 10% of β-cyclodextrin in distilled water. Kneading method and solvent evaporation method was use to prepared solid dispersion of aceclofenac and β-cyclodextrin. Different evaluation tests like solubility study in different solvents, PXRD and in vitro dissolution study of aceclofenac- β-cyclodextrin inclusion complex were carried out. The overall finding indicated that β-cyclodextrin is a desirable water soluble carrier, that helps in increasing solubility of drug. Due to its structural feature, β-cyclodextrin forms a good inclusion complex that decreases contact angle of drug with water molecules by increasing wetting properties. Hence, it can be concluded that, β-cyclodextrin is better water soluble carrier molecule in terms of its compatibility and increasing solubility behavior of poorly water soluble drug aceclofenac.

DEVELOPMENT AND EVALUATION OF ZIPRASIDONE LOADED SOLID SELF-MICRO EMULSIFYING DRUG DELIVERY SYSTEM

INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (08) ◽  
pp. 53-60
Author(s):  
Purushottam Patil ◽  
Malik Shaikh ◽  
Paresh Mahaparale
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Physical Adsorption ◽  
Gastrointestinal Transit ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Poorly Water Soluble

Solid self-micro emulsification technique is the new approach for poorly water-soluble and poorly bioavailable drugs by allowing the drug substance to be incorporated into the oil phase and thus having the ability to permeate the GI membrane to a faster extent. Oleic acid, Tween 80, methanol and colloidal silicon dioxide were used as penetrant, surfactant, co-surfactant and adsorbent, respectively. The interaction between drug and excipients was examined by differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). The results of DSC and FTIR studies did not reveal any possible drug-excipient interactions. The conversion of liquid self-microemulsifying drug delivery system (SMEDDS) into the solid SMEDDS increases the stability of the emulsion formulation achieved by physical adsorption of an adsorbent material. The release of drug from SMEDDS formulation is justified by in-vitro dissolution studies. SMEDDS increases the solubility of the drug and improves the bioavailability, without disturbing gastrointestinal transit. SMEDDS has the potential to provide a useful oral solid dosage form for the poorly water-soluble drug ziprasidone.

Medicated structural PVP/PEG composites fabricated using coaxial electrospinning

e-Polymers ◽  
2017 ◽  
Vol 17 (1) ◽  
pp. 39-44 ◽  
Author(s):  
Yong-Hui Wu ◽  
Deng-Guang Yu ◽  
Hai-Peng Li ◽  
Xiang-Yang Wu ◽  
Xiao-Yan Li
Keyword(s):  
Electron Microscope ◽  
Citric Acid ◽  
Shell Structure ◽  
Water Soluble ◽  
Working Fluid ◽  
Coaxial Electrospinning ◽  
Core Shell ◽  
The Core ◽  
Poorly Water Soluble ◽  
Core Shell Structure

AbstractA new type of medicated polymeric composite consisting of acyclovir (ACY), polyvinylpyrrolidone K60 (PVP) and polyethylene glycol 6000 (PEG) with core-shell structure were prepared by a coaxial electrospinning process. The composites could enhance the dissolution of the poorly water-soluble drug. The shell layers were formed from a spinnable working fluid containing the filament-forming PVP and citric acid while the core parts were prepared from an un-spinnable co-dissolving solution composed of ACY, sodium hydrate and PEG. Scanning electron microscope and transmission electron microscope observations demonstrated that the composites had a homogeneous linear topography with a slippery surface, a diameter of 670±130 nm, and an obvious core-shell structure. X-ray diffraction (XRD) and attenuated total reflectance-Fourier transform infrared (ATR-FTIR) spectroscopy results demonstrated that the drug and citric acid contained in the core and shell parts were in an amorphous status. In vitro dissolution experiments exhibited that ACY was able to be free within 1 min, and the dissolution media were neutral due to acid-basic action within the core-shell structures. The medicated nanocomposites resulted from a combined usage of hydrophilic polymeric excipients PVP and PEG could provide a new solution to the problem associated with the dissolution of poorly water-soluble drugs.

scholarly journals Amorphous solid dispersions and the confounding effect of nanoparticles in in vitro dissolution and in vivo testing: Niclosamide as a case of study

2020 ◽  
Author(s):  
Miguel O Jara ◽  
Zachary N Warnken ◽  
Robert O Williams
Keyword(s):  
Amorphous Solid ◽  
Fold Increase ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Amorphous Solid Dispersion ◽  
In Vitro Tests ◽  
Manufacturing Method ◽  
Poorly Water Soluble

We developed an amorphous solid dispersion (ASD) of the poorly water soluble molecule niclosamide that achieved more than a 2 fold increase in bioavailability. Notably, this niclosamide ASD formulation increased the apparent drug solubility about 60 fold relative to the crystalline material due to the generation of nanoparticles. Niclosamide is a weakly acidic drug, BCS class II, and a poor glass former with low bioavailability in vivo. Hot melt extrusion is a high throughput manufacturing method commonly used in the development of ASDs for increasing the apparent solubility and bioavailability of poorly water-soluble compounds. We utilized the polymer polyvinylpyrrolidone vinyl acetate (PVPVA) to manufacture niclosamide ASDs by extrusion. Samples were analyzed based on their microscopic and macroscopic behavior and their intermolecular interactions, using DSC, XRD, NMR, FTIR, and DLS. The niclosamide ASD generated nanoparticles with a mean particle size of about 100 nm in FaSSIF media. In a side by side diffusion test, these nanoparticles produced a 4 fold increase in niclosamide diffusion. We successfully manufactured amorphous extrudates of the poor glass former niclosamide that showed remarkable in vitro dissolution and diffusion performance. These in vitro tests were translated to a rat model that also showed an increase in oral bioavailability.

Design, Optimization and Evaluation of Repaglinide Self-Nanoemulsifying Drug Delivery for Enhanced Solubility

2017 ◽  
Vol 10 (6) ◽  
pp. 3920-3928
Author(s):  
Mahalaxmi K ◽  
Sailu Ch
Keyword(s):  
Drug Delivery ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Antidiabetic Drug ◽  
Water Soluble Drug ◽  
Enhanced Solubility ◽  
Poorly Water Soluble ◽  
Capmul Mcm ◽  
Poorly Water Soluble Drug

The aim of study was to develop self-nanoemulsifying systems of poorly water-soluble drug repaglinide, which is an antidiabetic drug in the class of medications known as meglitinides. Solubility of repaglinide in oily phases and surfactants was determined to identify components of self-nanoemulsifying drug delivery system (SNEDDS). Surfactants and oil was selected based on solubility studies were further screened for their efficiency in formulation. Acrysol K 150, Kolliphor EL and Capmul MCM were selected as oil, surfactant and co-surfactant respectively. Formulation F8 was found to be optimized formulation on the basis of in vitro dissolution studies, particle size and zeta potential. The optimized formulation was then subjected to stability studies and was found to be stable after 6 months. Thus, SNEDDS were found to be influential in improving the release performance of repaglinide, indicating their potential to improve the solubility and oral bioavailability of repaglinide.  

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