The effect of water solubility of solutes on their flux through human skin in vitro: A prodrug database integrated into the extended Flynn database

In intact skin the epidermal layer is a dynamic tissue component which is maintained by a basal layer of mitotically active cells. The protective upper epidermis, the stratum corneum, is generated by differentiation of the suprabasal keratinocytes which eventually desquamate as anuclear comeocytes. A similar sequence of events is observed in vitro in the non-contracting human skin equivalent (HSE) which was developed in this lab (1). As a part of the definition process for this model of living skin we are examining its ultrastructural features. Since desmosomes are important in maintaining cell-cell interactions in stratified epithelia their distribution in HSE was examined.

Download Full-text

Expression of intercellular adhesion molecule-1 in UVA-irradiated human skin cells in vitro and in vivo

British Journal of Dermatology ◽

10.1046/j.1365-2133.1996.d01-982.x ◽

1996 ◽

Vol 135 (2) ◽

pp. 241-247 ◽

Cited By ~ 1

Author(s):

G. TREINA ◽

C. SCALETTA ◽

A. FOURTANIER ◽

S. SEITE ◽

E. FRENK ◽

...

Keyword(s):

Human Skin ◽

Adhesion Molecule ◽

Intercellular Adhesion ◽

Intercellular Adhesion Molecule ◽

Intercellular Adhesion Molecule 1 ◽

Skin Cells ◽

Human Skin Cells

Download Full-text

Complexation with Hydroxypropyl-gama-Cyclodextrin of Birch Tree Extract Physico-chemical Characterisation of their Binary Products

Revista de Chimie ◽

10.37358/rc.08.6.1854 ◽

2008 ◽

Vol 59 (6) ◽

Cited By ~ 1

Author(s):

Codruta Soica ◽

Cristina A. Dehelean ◽

Valentin Ordodi ◽

Diana Antal ◽

Vicentiu Vlaia

Keyword(s):

Inclusion Complexes ◽

Water Solubility ◽

In Vitro Dissolution ◽

Molar Ratio ◽

Bark Extract ◽

Birch Bark ◽

Preparation Methods ◽

Birch Tree ◽

Physico Chemical

Birch bark contains important pentacyclic triterpens that determine an anticancer, anti-inflammatory and antiviral activity. The compounds can be extracted by simple procedures with organic solvents. The major problem of this type of triterpens is their low water solubility which can be increased by physical procedures like cyclodextrin complexation. The aim of present study was to analyse the products between birch bark extract and hydroxypropyl-g -cyclodextrin. Hydroxypropyl-g -cyclodextrin (HPGCD) was used as a host to improve its solubility in water, via inclusion complex formation. In order to obtain the inclusion complexes, 1:2 molar ratio and two preparation methods (physical mixing, kneading) were used. The inclusion complexes were analyzed by in vitro dissolution tests, thermal analysis and X-ray diffraction.

Download Full-text

Human Skin-Derived Fibroblasts Acquire In Vitro Anti-Tumor Potential after Priming with Paclitaxel

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520611313030015 ◽

2013 ◽

Vol 13 (3) ◽

pp. 523-530 ◽

Cited By ~ 1

Author(s):

Augusto Pessina ◽

Valentina Cocce ◽

Arianna Bonomi ◽

Loredana Cavicchini ◽

Francesca Sisto ◽

...

Keyword(s):

Human Skin

Download Full-text

Targeting Breast Cancer Cells with G4 PAMAM Dendrimers and Valproic Acid Derivative Complexes

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520620666200423073812 ◽

2020 ◽

Vol 20 (15) ◽

pp. 1857-1872

Author(s):

Alberto M. Muñoz ◽

Manuel J. Fragoso-Vázquez ◽

Berenice P. Martel ◽

Alma Chávez-Blanco ◽

Alfonso Dueñas-González ◽

...

Keyword(s):

Valproic Acid ◽

Cell Lines ◽

Water Solubility ◽

Md Simulations ◽

Pamam Dendrimer ◽

Pamam Dendrimers ◽

Force Microscopy ◽

Micromolar Concentration ◽

Atomic Force

Background: Our research group has developed some Valproic Acid (VPA) derivatives employed as anti-proliferative compounds targeting the HDAC8 enzyme. However, some of these compounds are poorly soluble in water. Objective: Employed the four generations of Polyamidoamine (G4 PAMAM) dendrimers as drug carriers of these compounds to increase their water solubility for further in vitro evaluation. Methods: VPA derivatives were subjected to Docking and Molecular Dynamics (MD) simulations to evaluate their affinity on G4 PAMAM. Then, HPLC-UV/VIS, 1H NMR, MALDI-TOF and atomic force microscopy were employed to establish the formation of the drug-G4 PAMAM complexes. Results: The docking results showed that the amide groups of VPA derivatives make polar interactions with G4 PAMAM, whereas MD simulations corroborated the stability of the complexes. HPLC UV/VIS experiments showed an increase in the drug water solubility which was found to be directly proportional to the amount of G4 PAMAM. 1H NMR showed a disappearance of the proton amine group signals, correlating with docking results. MALDI-TOF and atomic force microscopy suggested the drug-G4 PAMAM dendrimer complexes formation. Discussion: In vitro studies showed that G4 PAMAM has toxicity in the micromolar concentration in MDAMB- 231, MCF7, and 3T3-L1 cell lines. VPA CF-G4 PAMAM dendrimer complex showed anti-proliferative properties in the micromolar concentration in MCF-7 and 3T3-L1, and in the milimolar concentration in MDAMB- 231, whereas VPA MF-G4 PAMAM dendrimer complex didn’t show effects on the three cell lines employed. Conclusion: These results demonstrate that G4 PAMAM dendrimers are capableof transporting poorly watersoluble aryl-VPA derivate compounds to increase its cytotoxic activity against neoplastic cell lines.

Download Full-text

Development and Optimization of Sustained Release Moxifloxacin Hydrochloride Loaded Nanoemulsion for Ophthalmic Drug Delivery: A 32 Factorial Design Approach

Micro and Nanosystems ◽

10.2174/1876402912999200826111031 ◽

2020 ◽

Vol 12 ◽

Author(s):

Sagar R. Pardeshi ◽

Harshal A. Mistari ◽

Rakhi S. Jain ◽

Pankaj R. Pardeshi ◽

Rahul L. Rajput ◽

...

Keyword(s):

Drug Release ◽

Sustained Release ◽

Factorial Design ◽

Water Solubility ◽

Tween 80 ◽

Drug Release Profile ◽

Sustained Drug Release ◽

Bacterial Conjunctivitis ◽

Promising Alternative

Background: Moxifloxacin is a BCS class I drug used in the treatment of bacterial conjunctivitis and keratitis. Despite its high water solubility, it possesses limited bioavailability due to anatomical and physiological constraints associated with the eyes which required multiple administrations to achieve a therapeutic effect. Objective: In order to prolong drug release and to improve antibacterial efficacy for the treatment of bacterial keratitis and conjunctivitis, moxifloxacin loaded nanoemulsion was developed. Methods: The concentration of oil (oleic acid), surfactant (tween 80), and cosurfactant (propylene glycol) were optimized by employing a 3-level 2-factorial design of experiment for the development of nanoemulsion. The developed nanoemulsion was characterized by particle size distribution, viscosity, refractive index, pH, drug content and release, transmission electron microscopy (TEM), and antibacterial study. The compatibility of the drug with the excipients was accessed by Fourier transform infrared spectroscopy (FTIR). Result: The average globule size was found to be 198.20 nm. The TEM study reveals the globules were nearly spherical and are well distributed. In vitro drug release profile for nanoemulsion shown sustained drug release (60.12% at the end of 6 h) compared to drug solution, where complete drug released within 2 h. The antibacterial effectiveness of the drug-loaded nanoemulsion was improved against S. aureus compared with the marketed formulation. Conclusion: The formulated sustained release nanoemulsion could be a promising alternative to eye drop with improved patient compliance by minimizing dosing frequency with improved antibacterial activity.

Download Full-text

The Effect of Practolol, In Vitro Generated Metabolites of Practolol and Chemical Analogues on the Rate of Growth of Human Skin Fibroblasts

Alternatives to Laboratory Animals ◽

10.1177/026119298401200205 ◽

1984 ◽

Vol 12 (2) ◽

pp. 89-97

Author(s):

Graham R. Elliott ◽

H.E. Amos ◽

James W. Bridges

Keyword(s):

Human Skin ◽

Psoriasis Patient ◽

Skin Fibroblasts ◽

Human Skin Fibroblasts ◽

Cell Type ◽

Normal Human Skin ◽

Rate Of Growth ◽

Structural Analogues ◽

Normal Human

The rate of growth of normal human skin fibroblasts was inhibited in a dose related, reversible, fashion by practolol (N-4-(2-hydroxy)-3 (1-methyl)-aminopropoxyphenylacetamine) (ID50 1.35 ± 0.14 x 10-3M), propranolol (1-(isopropylamino)-3(1-naphthyl-oxy)-2-propranolol) (ID50 0.145 ± 0.02 x 10-3M) and paracetamol (N-(4-hydroxyphenyl) acetamide) (ID50 0.85 ± 0.2 x 10-3M). Skin fibroblasts isolated from a psoriasis patient were more sensitive towards practolol (ID50 0.48 ± 0.14 x 10-3M) and propranolol (ID50 0.032 ± 0.002 x 10-3M), but less sensitive towards paracetamol (ID50 1.3 ± 0.07 x 10-3M). In vitro generated metabolites of practolol, using normal or Arochlor 1254-pretreated hamster liver preparations, and structural analogues of practolol had no effect upon the growth of either cell type.

Download Full-text

Optimization of the preparation process of mung bean puffed infant rice cereal and evaluation of the structure and digestion characteristics of starch

International Journal of Food Engineering ◽

10.1515/ijfe-2020-0025 ◽

2020 ◽

Vol 16 (8) ◽

Author(s):

Jiabao Cao ◽

Baoxin Lu ◽

Dongjie Zhang ◽

Longkui Cao ◽

Xia Wang ◽

...

Keyword(s):

Mung Bean ◽

Water Solubility ◽

Raw Materials ◽

Xrd Analysis ◽

Particle Structure ◽

Screw Speed ◽

Nutrient Analysis ◽

Shaped Particle ◽

Feed Moisture

AbstractThe present study was carried out to produce a high quality puffed infant rice cereal from rice and mung bean through extrusion technology. Experiments were designed using 3 independent variables (i. e. 14–18% feed moisture, 400–550 r/min screw speed and 125–175 °C barrel temperature) and 3 response variables (i. e. bulk density, water solubility index and degree of gelatinisation) at five different levels of central composite rotatable design (CCRD). The results of optimization demonstrated that 14% feed moisture, 400 r/min screw speed and 175 °C barrel temperature could generate rice-mungbean extrudates with desirable functional properties. The selected extrudate samples were further examined using scanning electron microscope (SEM), rapid viscosity analyzer (RVA), Fourier transform infrared spectrometer (FTIR), X-ray diffraction (XRD) analysis, in vitro digestibility and fundamental nutrient analysis. Notably, the initial oval-shaped particle structure of starch in the raw materials disappeared, the surface debris and roughness increased, and the density decreased. The time required for the gelatinization of puffed infant rice cereal was the shortest, which was in agreement with the positioning of ready-to-eat weaning food for infants. Moreover, the puffed infant rice cereal displayed higher peak viscosity and breakdown value, smaller retrogradation value and greater top taste value compared to the commercial infant rice cereal. Besides maintaining the initial characteristic peak of starch, the puffed infant rice cereal demonstrated characteristic absorption peaks of COO- in the vicinity of 1546 cm−1 and 1437 cm−1, indicating the formation of carboxylate during extrusion. In addition, the puffed infant rice cereal exhibited firm diffraction peaks at the diffraction angles of 7.4°, 12.5° and 20.5°, indicating that a certain amount of starch changed from type A to type V. Furthermore, the digestive rate of puffed infant rice cereal was higher than that of commercial infant cereal (90.21 versus 86.96%, respectively; p < 0.05). Altogether, our findings reveal that the developed puffed infant rice cereal meets the standards set by the Codex Alimentarius Commission (CAC; 74-1981).

Download Full-text