Saquinavir-Piperine Eutectic Mixture: Preparation, Characterization, and Dissolution Profile.

The dissolution rate of the anti-HIV drug saquinavir base (SQV), a poorly water-soluble and extremely low absolute bioavailability drug, was improved through a eutectic mixture formation approach. A screening based on a liquid-assisted grinding technique was performed using a 1:1 molar ratio of the drug and the coformers sodium saccharinate, theobromine, nicotinic acid, nicotinamide, vanillin, vanillic acid, and piperine (PIP), followed by differential scanning calorimetry (DSC). Given that SQV-PIP was the only resulting eutectic system from the screening, both the binary phase and the Tammann diagrams were adapted to this system using DSC data of mixtures prepared from 0.

Curcumin Hybrid Lipid Polymeric Nanoparticles: Antioxidant Activity, Immune Cellular Response, and Cytotoxicity Evaluation.

Poor solubility and short biological half-life present a challenge that needs to be overcome in order to improve the recognized bioactivities of curcumin (CUR), the main phenolic compounds derived from the roots of . However, drug delivery systems have proven to be an excellent strategy to improve and obtain greater bioavailability. Our previous studies on curcuminoid hybrid nanoparticles have shown promising results by significantly increasing the solubility of desmethoxycurcumin (DMC) and bisdemethoxycurcumin (BDM).

Hybrid Nanoparticles of Proanthocyanidins from Leaves: QTOF-ESI MS Characterization, Antioxidant Activity and Immune Cellular Response.

Previous studies in have shown promising results concerning the characterization of polyphenols with leaves yielding more diverse proanthocyanidins and higher bioactivities values. However, the polyphenols-microbiota interaction at the colonic level and their catabolites avoid the beneficial effects that can be exerted by this medicinal plant when consumed. In this regard, a new generation of hybrid nanoparticles has demonstrated improvements in natural compounds' activity by increasing their bioavailability.

Bovine Serum Albumin-Based Nanoparticles: Preparation, Characterization, and Antioxidant Activity Enhancement of Three Main Curcuminoids from .

Bovine Serum Albumin (BSA) lipid hybrid nanoparticles are part of the new solutions to overcome low bioavailability of poor solubility drugs such as curcuminoids, which possess multiple biological advantages; however, they are counterbalanced by its short biological half-life. In this line, we prepared the three main curcuminoids: curcumin (CUR), desmethoxycurcumin (DMC), and bisdemethoxycurcumin (BDM)-loaded BSA nanoparticles. The three formulations were characterized by the average size, size distribution, crystallinity, weight loss, drug release, kinetic mechanism, and antioxidant activity.

Evaluation of Piperine as Natural Coformer for Eutectics Preparation of Drugs Used in the Treatment of Cardiovascular Diseases.

Piperine (PIP) was evaluated as a natural coformer in the preparation of multicomponent organic materials for enhancing solubility and dissolution rate of the poorly water-soluble drugs: curcumin (CUR), lovastatin (LOV), and irbesartan (IBS). A screening based on liquid assisted grinding technique was performed using 1:1 drug-PIP molar ratio mixtures, followed by differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) analyses. Three eutectic mixtures (EMs) composed of CUR-PIP, LOV-PIP, and IBS-PIP were obtained.

Interaction and Compatibility Studies in the Development of Olmesartan Medoxomil and Hydrochlorothiazide Formulations under a Real Manufacturing Process.

A drug-drug and drug-excipient interactions and compatibilities study was conducted for two fixed-dose combination (FDC) products containing olmesartan medoxomil (OLM)/hydrochlorothiazide (HCT) 20/12.5 mg and OLM/HCT 40/12.5 mg during their development including storage.

A New Saquinavir Mesylate-Sodium Decyl Sulfate Salt Discovered by Serendipity during an Anomalous Dissolution Test.

Purpose: To understand the anomalous behavior of Saquinavir Mesylate (SQVM) in sodium decyl sulfate (SDS) medium during a dissolution test through a crystallographic analysis of the crystal obtained. As a result, it will be possible to elucidate its crystal structure and carry out a complete solid-state characterization of the API.

Methods: The solid form obtained was characterized by a structural analysis through X-ray single crystal and powder diffraction.

Design of Hybrid Polymeric-Lipid Nanoparticles Using Curcumin as a Model: Preparation, Characterization, and In Vitro Evaluation of Demethoxycurcumin and Bisdemethoxycurcumin-Loaded Nanoparticles.

Polymeric lipid hybrid nanoparticles (PLHNs) are the new generation of drug delivery systems that has emerged as a combination of a polymeric core and lipid shell. We designed and optimized a simple method for the preparation of Pluronic F-127-based PLHNs able to load separately demethoxycurcumin (DMC) and bisdemethoycurcumin (BDM). CUR was used as a model compound due to its greater availability from turmeric and its structure similarity with DMC and BDM.

Use of nanosystems to improve the anticancer effects of curcumin.

Curcumin (CUR) is a phenolic compound that is safe for human consumption. It exhibits chemopreventive, antiproliferative, antiangiogenic, and antimetastatic effects. However, these benefits can be hampered due to the lipophilic nature, rapid metabolism, low bioavailability, and fast elimination of the molecule.

Curcumin Loaded and Co-loaded Nanosystems: A Review from a Biological Activity Enhancement Perspective.

Background: Curcumin is a natural phenolic compound exhibiting multiple bioactivities that have been evaluated in vitro, in vivo as well as through clinical studies in humans. Some of them include antimicrobial, antioxidant, anti-inflammatory, and central nervous system protective effects. Further, curcumin is generally recognized as a safe substance because of its low toxicity.

Irbesartan desmotropes: Solid-state characterization, thermodynamic study and dissolution properties.

Irbesartan (IBS) is a tetrazole derivative and antihypertensive drug that has two interconvertible structures, 1H- and 2H-tautomers. The difference between them lies in the protonation of the tetrazole ring. In the solid-state, both tautomers can be isolated as crystal forms A (1H-tautomer) and B (2H-tautomer).

Drug Solubility Enhancement through the Preparation of Multicomponent Organic Materials: Eutectics of Lovastatin with Carboxylic Acids.

Lovastatin (LOV) is a drug used to treat hypercholesterolemia. Recent studies have identified its antioxidant effects and potential use in the treatment of some types of cancer. However, the low bioavailability related to its poor water solubility limits its use in solid oral dosage forms.

The effect of solution environment and the electrostatic factor on the crystallisation of desmotropes of irbesartan.

The experimental conditions necessary for stabilising irbesartan (IBS) tautomers in solution and selectively obtaining the desmotropic crystal forms are presented herein. 1H and 2H tautomers were stabilized in specific solution conditions and the 2H-tetrazole⋯imidazole interaction was confirmed by solution-state NMR. The results showed that highly polar and polarisable solvents (higher values of the electrostatic factor (EF)) lead to the crystallisation of IBS form B.

Crystallization of progesterone polymorphs using polymer-induced heteronucleation (PIHn) method.

Progesterone is a natural hormone steroid used in humans for several treatments and in livestock for artificial insemination, which exhibits two polymorphic forms at ambient conditions: form 1 and form 2. Form 2 is metastable and more soluble than form 1; however, it is not suitable to use as powder raw material because it transforms into form 1 by the effects of grinding. A polymorphic screening of progesterone based on polymer-induced heteronucleation method was performed as an alternative to prepare the metastable form.

Dissolution properties, solid-state transformation and polymorphic crystallization: progesterone case study.

Progesterone is a natural steroid hormone and a poor soluble drug which presents two polymorphs (forms 1 and 2). Different methods to obtain form 2 were tested and a complete solid-state characterization of both polymorphs (forms 1 and 2) was conducted. X-ray powder diffraction, hot stage microscopy, Fourier transform infrared, dispersive Raman, (13)C solid-state nuclear magnetic resonance spectroscopy, thermal analysis, scanning electron microscopy techniques and intrinsic dissolution rates (IDR) were applied to investigate physical-chemical and dissolution properties of these two polymorphs.

Morphology study of progesterone polymorphs prepared by polymer-induced heteronucleation (PIHn).

In this article, morphology of progesterone polymorphs prepared by polymer-induced heteronucleation (PIHn) technique was studied. Hydroxypropyl methylcellulose(HPMC), such as dextran T-500 and gelatin G-9382, polyisoprene (PI), and acrylonitrile/butadiene copolymer (NBR) were used as substrates. The crystallizations were performed by solvent evaporation at room temperature from 0.