Solubilization of poorly water‐soluble bioactive molecules in neutral aqueous media by complexation with renatured β‐1,3‐1,6‐glucan nanoparticles

Biopolymers ◽  
2020 ◽  
Vol 111 (4) ◽  
Author(s):  
Ayumu Kodama ◽  
Akifumi Nakagawa ◽  
Yuki Nonoguchi ◽  
Haruka Sakurai ◽  
Chieko Yano ◽  
...  
Keyword(s):  
Aqueous Media ◽  
Water Soluble ◽  
Bioactive Molecules ◽  
Poorly Water Soluble

Aqueous Solubilization of Paclitaxel Using Hydrotropic Polymer Micelle

2007 ◽  
Vol 342-343 ◽  
pp. 421-424 ◽  
Author(s):  
Hyun Su Min ◽  
Hong Jae Lee ◽  
Sang Cheon Lee ◽  
Kyoung Hoon Kang ◽  
Jae Hwi Lee ◽  
...  
Keyword(s):  
Polymer Concentration ◽  
Aqueous Media ◽  
Water Soluble ◽  
Polymer Micelle ◽  
Water Soluble Drug ◽  
Poorly Soluble ◽  
Poorly Water Soluble ◽  
Poly Ethylene ◽  
Hydrotropic Agent ◽  
Poorly Water Soluble Drug

Hydrotropic block copolymers, consisting of a hydrophilic poly(ethylene glycol) (PEG) block and a hydrotropic polymer, poly(2-(4-(vinyl benzyloxy)-N,N-diethylnicotinamide)) [P(VBODENA)], block, were synthesized by atom transfer radical polymerization (ATRP) for aqueous solubilization of paclitaxel, a representative poorly water-soluble drug. These polymers showed an excellent solubilizing effect for paclitaxel in aqueous media in comparison with the corresponding hydrotropic agent and a control micelle (PEG-PLA) and such effect was significantly dependent on the polymer concentration and composition. Paclitaxel could be solubilized into polymer micelles in aqueous media without use of an organic solvent. Due to their promising properties such as micellar characteristics and hydrotropic solubilization, the hydrotropic polymer micelle system can be useful for formulation of paclitaxel and other poorly soluble drugs.

Electrospraying as a novel process for the synthesis of particles/nanoparticles loaded with poorly water-soluble bioactive molecules

2021 ◽  
Vol 290 ◽  
pp. 102384
Author(s):  
Hadis Rostamabadi ◽  
Seid Reza Falsafi ◽  
Mohammad Mahdi Rostamabadi ◽  
Elham Assadpour ◽  
Seid Mahdi Jafari
Keyword(s):  
Water Soluble ◽  
Bioactive Molecules ◽  
Poorly Water Soluble

scholarly journals Sustained absorption of delamanid from lipid-based formulations as a path to reduced frequency of administration

2020 ◽  
Author(s):  
Gisela Ramirez ◽  
Anna C. Pham ◽  
Andrew J. Clulow ◽  
Malinda Salim ◽  
Adrian Hawley ◽  
...  
Keyword(s):  
Self Assembly ◽  
Aqueous Suspension ◽  
Aqueous Media ◽  
Milk Powder ◽  
Water Soluble ◽  
Selachyl Alcohol ◽  
Self Assembling ◽  
Suspension Formulation ◽  
Poorly Water Soluble ◽  
Reconstituted Milk

Abstract Delamanid is a poorly water-soluble drug currently being used for the treatment of tuberculosis. The high frequency of dosing leads to poor adherence for patients who live in lower economic and nomadic populations. Non-digestible self-assembling lipids as a formulation approach for poorly water-soluble drugs have previously been shown to extend the window of absorption through gastric retention. We hypothesise that this approach could lead to the reduction of dosing frequency for delamanid and thereby has potential to improve adherence. Formulations of delamanid were prepared in selachyl alcohol and phytantriol as non-digestible self-assembling lipid vehicles, and their behaviour was compared with reconstituted milk powder, as a digestible lipid-based formulation, and an aqueous suspension. The self-assembly of selachyl alcohol and phytantriol in aqueous media in the presence of delamanid was studied using small angle X-ray scattering and produced the inverse hexagonal (H2) and inverse bicontinuous cubic (V2) liquid crystal structures, respectively. The times at which maximum delamanid levels in plasma were observed (Tmax) after oral administration of the phytantriol, selachyl alcohol and reconstituted milk powder formulations of delamanid to rats were 27 ± 3, 20 ± 4 and 6.5 ± 1.0 h, respectively, compared with the aqueous suspension formulation with a Tmax of 3.4 ± 1 h, which confirms the hypothesis of an extended duration of absorption after administration in non-digestible self-assembling lipids. The digestion products of the triglycerides in the milk formulation increased the solubilisation of delamanid in the gastrointestinal tract, leading to an increase in exposure compared with the aqueous suspension formulation but did not significantly extend Tmax. Overall, the non-digestible nanostructured lipid formulations extended the duration of absorption of delamanid well beyond that from milk or suspension formulations.

Behaviour of Lipid-Based Formulations Containing Nifedipine in Aqueous Media as Observed by Small Angle X-Ray Scattering

2013 ◽  
Vol 747 ◽  
pp. 139-142 ◽  
Author(s):  
Yotsanan Weerapol ◽  
Mont Kumpugdee-Vollrath ◽  
Pornsak Sriamornsak
Keyword(s):  
Small Angle ◽  
Castor Oil ◽  
Aqueous Media ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Simulated Gastric Fluid ◽  
X Ray ◽  
X Ray Scattering ◽  
Poorly Water Soluble ◽  
Ray Scattering

Lipid-based formulations (LBF) including self-emulsifying drug delivery system have been used to improve drug dissolution and bioavailability by avoiding rate-limiting step during dissolution of poorly water-soluble drugs. This study was aimed to investigate the behavior of lipid-based formulations upon dilution in aqueous media by using small angle X-ray scattering (SAXS). LBF is composed of oil (caprylic/capric glyceride), surfactants (polyoxyl 35 castor oil or polyoxyl 40 hydrogenated castor oil), and co-solvent (diethylene glycol monoethyl ether) at a weight ratio of 1:1:8. Nifedipine, a poorly water-soluble drug, was used as a model drug. A 100-fold dilution of the LBF in aqueous media (i.e., simulated gastric fluid USP without pepsin (SGF) and distilled water) resulted in nanosized emulsion (less than 200 nm). The selected formulations were diluted in aqueous media at various ratios (e.g., 0.01, 0.02, 0.04, 0.06, 0.09, 0.11, 0.18, 0.25, 0.67, 1.5, 4, 99, 199 and 300 folds) and then, after equilibrium, monitored by SAXS in order to observe the surfactant rearrangement. The results from SAXS scattering curves (qof 0.027-0.980 Å-1) demonstrated that a lamellar phase or liquid crystalline was not formed upon dilution. The emulsions were formed without the ordered structure.

NANO-SIZED SOLID DISPERSION OF A POORLY WATER-SOLUBLE DRUG

2012 ◽  
pp. 31-35
Author(s):  
Truong Dinh Thao Tran ◽  
Ha Lien Phuong Tran ◽  
Nghia Khanh Tran ◽  
Van Toi Vo
Keyword(s):  
Drug Release ◽  
Droplet Size ◽  
Solid Dispersion ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Dissolution Enhancement ◽  
Particle Size Reduction ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Purposes: Aims of this study are dissolution enhancement of a poorly water-soluble drug by nano-sized solid dispersion and investigation of machenism of drug release from the solid dispersion. A drug for osteoporosis treatment was used as the model drug in the study. Methods: melting method was used to prepare the solid dispersion. Drug dissolution rate was investigated at pH 1.2 and pH 6.8. Drug crystallinity was studied using differential scanning calorimetric and powder X-ray diffraction. In addition, droplet size and contact angle of drug were determined to elucidate mechanism of drug release. Results: Drug dissolution from the solid dispersion was significantly increased at pH 1.2 and pH 6.8 as compared to pure drug. Drug crystallinity was changed to partially amorphous. Also dissolution enhancement of drug was due to the improved wettability. The droplet size of drug was in the scale of nano-size when solid dispersion was dispersed in dissolution media. Conclusions: nano-sized solid dispersion in this research was a successful preparation to enhance bioavailability of a poorly water-soluble drug by mechanisms of crystal changes, particle size reduction and increase of wet property.

Enhancement of Solubility and Dissolution Rate of Poorly Water Soluble Drug using Cosolvency and Solid Dispersion Techniques

1970 ◽  
Vol 1 (4) ◽  
pp. 349-356
Author(s):  
Meka Lingam ◽  
Vobalaboina Venkateswarlu
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersions ◽  
Physicochemical Characterization ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
Peg 400 ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

The low aqueous solubility of celecoxib (CB) and thus its low bioavailability is a problem.    Thus, it is suggested to improve the solubility using cosolvency and solid dispersions techniques. Pure CB has solubility of 6.26±0.23µg/ml in water but increased solubility of CB was observed with increasing concentration of cosolvents like PEG 400, ethanol and propylene glycol. Highest solubility (791.06±15.57mg/ml) was observed with cosolvency technique containing the mixture of composition 10:80:10%v/v of water: PEG 400: ethanol. SDs with different polymers like PVP, PEG were prepared and subjected to physicochemical characterization using Fourier-transform infrared (FTIR) spectroscopy, X-ray diffractometry (XRD), differential scanning calorimetry (DSC), solubility and dissolution studies. These studies reveals that CB exists mainly in amorphous form in prepared solid dispersions of PVP, PEG4000 and PEG6000 further it can also be confirmed by solubility and dissolution rate studies. Solid dispersions of PV5 and PV9 have shown highest saturation solubility and dissolution rate

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