Matrix Forming Behavior of Doxycycline Hyclate-Loaded Beta-Cyclodextrin In Situ Forming Matrix and Microparticle

2019 ◽  
Vol 819 ◽  
pp. 221-226 ◽  
Author(s):  
Nutdanai Lertsuphotvanit ◽  
Pornsit Chaiya ◽  
Thawatchai Phaechamud
Keyword(s):  
Surface Tension ◽  
Contact Angle ◽  
Particle Size ◽  
Delivery System ◽  
Aqueous Environment ◽  
Doxycycline Hyclate ◽  
Beta Cyclodextrin ◽  
Internal Phase ◽  
External Phase

In situ forming microparticle (ISM) is an injectable emulsion drug delivery system comprising drug loaded in polymeric solution as internal phase and oil combined with emulsifier as external phase. This emulsion transforms into microparticle after contact an aqueous environment by solvent exchange mechanism. This study developed ISM using internal phase comprising 5% w/w doxycycline hyclate (DH) loaded with various concentrations of beta-cyclodextrin (β-CD) using N-methyl-2-pyrrolidone (NMP) as a solvent and external phase containing olive oil combined with glyceryl monostearate (GMS). High concentrated β-CD solutions in NMP are used as the internal phase of ISM. Matrix forming behavior is evaluated for their particle size, transformation to microparticle, pH, rate of matrix formation, contact angle and surface tension. Each emulsion had similar pH values about 3.5-4.1 and transformed into microparticles (particle size about 60 μm) after contact with phosphate buffer pH 6.8. The particle sizes of each preparation decreased significantly after transformed into microparticles and the more microparticles were evident with time. The rate of matrix formation of ISM was apparent slower than its internal phase and was slower with time. Contact angle of ISM and its internal phase showed good wetting which the surface tension of 35% w/w β-CD ISM was 44.19 mN/m. The β-CD ISM exhibited as the potential delivery system for incorporation of active compounds.

Phase Inversion-Induced Rosin In Situ Forming Matrix Using Various Organic Biocompatible Solvents for Periodontitis Treatment

2020 ◽  
Vol 856 ◽  
pp. 237-244
Author(s):  
Nutdanai Lertsuphotvanit ◽  
Jongjan Mahadlek ◽  
Sarun Tuntarawongsa ◽  
Thawatchai Phaechamud
Keyword(s):  
Drug Delivery ◽  
Surface Tension ◽  
Antimicrobial Agent ◽  
Dimethyl Sulfoxide ◽  
Drug Delivery System ◽  
Delivery System ◽  
Phase Inversion ◽  
Contact Angles ◽  
Formation Behavior

In situ forming matrix (ISM) is an injectable drug delivery system containing a drug-loaded polymeric solution. It was applied for local drug administration such as into a periodontal pocket for periodontitis treatment with an antimicrobial agent. ISM can transform with phase inversion into the solid-like matrix after contact an aqueous environment by solvent exchange mechanism. This study aims to develop ISM which various concentrations of rosin (R) as matrix former dissolved in organic biocompatible and biodegradable solvents such as N-methyl-2-pyrrolidone, dimethyl sulfoxide and 2-pyrrolidone. Physicochemical characterization and matrix formation behavior owing to phase inversion of R ISM were evaluated including pH, density, viscosity, contact angles, surface tension, expelling force through a syringe, matrix formation behavior and morphological change. The density of all R ISM exhibited in the range of 1.03-1.11 g/cm3 and contact angles (9.04-44.13°) indicated a good wetting property. Higher R concentration decreased pH of ISM owing to increased amount of abietic and pimaric acid from R while the viscosity, contact angles and force for expelling a syringe were increased. The viscosity of R ISM in dimethyl sulfoxide was less than that in 2-pyrrolidone; thus, ISM using dimethyl sulfoxide as a solvent exhibited good injectability. ISM comprising R concentration > 30%w/w promoted a faster matrix growth in which the amount of occurred R matrix was enhanced with time and the rate of matrix formation was lower with time. Doxycycline Hyclate (Dx)-loaded 40%w/w ISM in dimethyl sulfoxide (Dx-DR) had pH of 3.70, density of 1.1084 ± 0.0005 g/ml, viscosity of 35.72 ± 0.00 cPs, contact angles of 26.87 ± 2.40°, surface tension of 37.11 ± 0.11 mN/m and expelling force of 23.98 ± 0.18 N. It showed the sustainable Dx release in simulated crevicular fluid and the efficient antimicrobial activity against Staphylococcus aureus and Porphyromonas gingivalis. Thus, this phase inversion induced R ISM using dimethyl sulfoxide as a solvent showed potential as an antimicrobial agent-loaded drug delivery system for periodontitis treatment.

Bleached Shellac as an Alternative Polymeric Matrix for In Situ Microparticle

2015 ◽  
Vol 659 ◽  
pp. 8-12
Author(s):  
Pitsiree Praphanwittaya ◽  
Thawatchai Phaechamud
Keyword(s):  
Droplet Size ◽  
Phosphate Buffer ◽  
Emulsion Droplet ◽  
Doxycycline Hyclate ◽  
Glyceryl Monostearate ◽  
Natural Resin ◽  
Regular Shape ◽  
External Phase ◽  
Bleached Shellac

Bleached shellac (BS), a biodegradable natural resin purified from insect lac, has been used in a varity of controlled drug delivery systems. Nevertheless, there were negligible researches explored the potential of it as in injectable in situ microparticles (ISM) applications. The goal of this study was to utilize BS to form ISM (shellac-solution dispersed into an external olive oil phase, as o/o emulsion) prepared by two-syringe technique. Addition of glyceryl monostearate (GMS) as stabilizer obviously decreased the emulsion droplet size. ISM emulsion comprising 5% w/w GMS in external phase could form into droplets and precipitate in form of microparticles after exposure to phosphate buffer. 2-Pyrrolidone was the most appropriate solvent to form massive microparticles with regular shape especially at ratio of 7:3 external:internal phases. ISM transformation was occurred after exposure to phosphate buffer and tended to reduce the droplet size when ratio of external phase was higher than 50%. Incorporation of doxycycline hyclate did not influence the amount and size of ISM. Therefore shellac exhibited as an alternative polymer matrix for ISM which higher amount of GMS could reduce the size of emulsion droplet and volume phase ratio seriously influenced on emulsion size and ISM formation.

Phase Behavior of Doxycycline Hyclate-Incorporated Bleached Shellac In Situ Forming Gel/Microparticle after Solvent Movement

2020 ◽  
Vol 859 ◽  
pp. 21-26
Author(s):  
Setthapong Senarat ◽  
Juree Charoenteeraboon ◽  
Pitsiree Praphanwittaya ◽  
Thawatchai Phaechamud
Keyword(s):  
Phase Behavior ◽  
Periodontal Pocket ◽  
Dense Matrix ◽  
Doxycycline Hyclate ◽  
Solvent Type ◽  
External Phase ◽  
The Matrix ◽  
Methyl Pyrrolidone ◽  
Bleached Shellac

With regard to the periodontal pocket application of in situ forming systems, the understanding the phase behavior after solidification owing to solvent movement could verify the deformability of specimen and its capacity to reside in the artificial periodontal pocket. The aim of this research was to investigate the phase behavior by determining mechanical properties as hardness and elasticity/plasticity ratio with texture analyzer for matrices obtained from drug-free and doxycycline hyclate (DX)-incorporated bleached shellac (BS) in situ forming gel (isg) and –microparticle (ism) after solvent exchange. The solvents for dissolving BS were 2-pyrrolidone (PYR), N-methyl pyrrolidone (NMP) and dimethyl sulfoxide (DMSO). The matrix from isg was less rough and bulge than that of isg. The order of mechanical hardness of transformed system prepared with different solvents was presented as PYR > NMP > DMSO, influenced by phase separation rate and porosity. The systems prepared with NMP and DMSO were more likely plastic or able to adapt its geometry to dynamic changes while that prepared with PYR was elastic. DX-incorporated ism matrix was still governed by the oil in external phase; thus, its consequence was reasonably plastic instead. XRD pattern indicated that the solvent type had no effect on the crystallinity of remained BS after solvent movement. SEM topography revealed sponge-like structure of isg prepared with DMSO and NMP whereas that prepared with PYR exhibited only initiated diminutive pores. The size and density of pores increased by time of isg using different solvents as following DMSO > NMP > PYR, whereas ism matrices had less pore density. The level of porosity of each matrix reflected the mechanical strength that a higher porous structure collapsed easily but a dense matrix considerably resisted to a compression.

Comparison of Doxycycline Hyclate Release from Beta-Cyclodextrin Based In Situ Forming Systems for Periodontal Pocket Targeting

2020 ◽  
Vol 859 ◽  
pp. 120-124
Author(s):  
Sarun Tuntarawongsa ◽  
Jongjan Mahadlek ◽  
Nutdanai Lertsuphotvanit ◽  
Thawatchai Phaechamud
Keyword(s):  
Drug Release ◽  
Direct Contact ◽  
Periodontal Pocket ◽  
Contact Method ◽  
Order Kinetic ◽  
Release Behavior ◽  
Doxycycline Hyclate ◽  
Factors Affecting ◽  
Beta Cyclodextrin

The release behavior of doxycycline hyclate (DH) from beta-cyclodextrin (β-CD) in situ gels (ISG) and in situ microparticles (ISM) was investigated using dialysis tube method and direct contact method compared to that from DH solution. From dialysis tube method, DH released completely from solution within 8 h, while it released with more sustainable from ISM and ISG completely at 12 h and 28 h, respectively. The release pattern of them was similar when tested using direct contact method (released completely at 9 days). The DH release from dialysis tube method of all systems was a first order kinetic. DH release from ISM using direct contact method fitted well with a Higuchi’s equation. The dialysis tube method was suitable for determining formula factors affecting the drug release behavior. However, to simulate the pocket condition with contact area is limited, the drug release test with direct contact method was preferred than dialysis tube method.

Mixed Solvent-Lauric Acid Solvent-Exchange Induced In Situ Forming Gel

2019 ◽  
Vol 819 ◽  
pp. 195-201
Author(s):  
Takorn Chantadee ◽  
Wichai Santimaleeworagun ◽  
Yaowaruk Phorom ◽  
Thawatchai Phaechamud
Keyword(s):  
Surface Tension ◽  
Contact Angle ◽  
Lauric Acid ◽  
Mixed Solvent ◽  
Mixed Solvents ◽  
Antimicrobial Activities ◽  
Solvent Mixture ◽  
High Ratio ◽  
Solvent Exchange

Designing lauric acid (L) solvent-exchange induced in situ forming gel (ISG) was conducted in this study by using mixed solvents (N-methyl pyrrolidone (NMP), 2-pyrrolidone (PYR) and dimethyl sulfoxide (DMSO) at different ratios. The pH, density, viscosity, matrix formation, contact angle/surface tension and antimicrobial activities of 50% w/w L in mixed solvents were determined. The pH and density of solvent decreased apparently with L addition. More amount of PYR in the solvent mixture increased the density and viscosity. High viscous manner of PYR resulted in the high surface tension and contact angle. The solvent mixture of NMP/PYR promoted a higher contact angle than the other mixed solvent systems. L in DMSO, PYR or solvent mixture with high ratio of DMSO or PYR transformed into matrix-like rapidly while those in NMP or high ratio of NMP had slower matrix formation after exposure to aqueous fluid. NMP and PYR showed antimicrobial activities effectively against all test microbes while L matrix retarded their activities. The mixed solvent concept is interesting to use for designing ISG comprising L as matrix former to prolong the drug release.

scholarly journals Is an electric field always a promoter of wetting? Electro-dewetting of metals by electrolytes probed by in situ X-ray nanotomography

2017 ◽  
Vol 199 ◽  
pp. 101-114 ◽  
Author(s):  
Maryana I. Nave ◽  
Yu Gu ◽  
Yu-Chen Karen Chen-Wiegart ◽  
Jun Wang ◽  
Konstantin G. Kornev
Keyword(s):  
Surface Tension ◽  
Contact Angle ◽  
Quantitative Analysis ◽  
Electric Field ◽  
Applied Electric Field ◽  
Electrochemical Cell ◽  
Reaction Products ◽  
X Ray ◽  
Electrolyte Surface

We developed a special electrochemical cell enabling quantitative analysis and in situ X-ray nanotomography of metal/electrolyte interfaces subject to corrosion. Using this cell and applying the nodoid model to describe menisci formed on tungsten wires during anodization, the evolution of the electrolyte surface tension, the concentration of reaction products, and the meniscus contact angle were studied. In contrast to the electrowetting effect, where the applied electric field decreases the contact angle of electrolytes, anodization of the tungsten wires increases the contact angle of the meniscus. Hence, an electric field favors dewetting rather than wetting of the newly formed surface. The discovered effect opens up new opportunities for the control of wetting phenomena and calls for the revision of existing theories of electrowetting.

scholarly journals THE USE OF Cyperus kyllinga EXTRACT IN SYNTHESIS OF SILVER NANOPARTICLE TO ENHANCE QUALITY OF GOAT LEATHER

2020 ◽  
Vol 17 (36) ◽  
pp. 159-170
Author(s):  
Eli ROHAETI ◽  
Nur Isna Melati PUTRI ◽  
Kun Sri BUDIASIH ◽  
Anna RAKHMAWATI
Keyword(s):  
Mechanical Properties ◽  
Contact Angle ◽  
Particle Size ◽  
Silver Nanoparticles ◽  
Tensile Strength ◽  
Silver Nanoparticle ◽  
Ex Situ ◽  
E Coli ◽  
In Situ Method

Improving leather quality with antifungal, antibacterial, and superior mechanical properties is an ongoing effort. The objectives of this research were to synthesize silver nanoparticle using Cyperus kyllinga extract as a bio-agent and to deposit synthesized silver nanoparticle into goat leather by ex situ and in situ, and also to characterize the properties of antibacterial, antifungal, mechanical, and contact angle of goat leather before and after modification. Preparation of silver nanoparticles by reduction method by adding Cyperus kyllinga’s leaf extract. The silver nanoparticle was characterized by using spectrophotometer UltraViolet-Visible and Particle Size Analyzer. The addition of Methyltrimethoxysilane (MTMS) compound on the leather sample to know hydrophobicity properties of the leather. The leather was modified by adding silver nanoparticle and silane compounds. The antibacterial and antifungal test was conducted by the diffusion method and tested the significance by using statistical analysis. The mechanical properties were tested through tensile strength test, elongation, and also modulus Young by using a tensile tester. The modified goat leather surface was tested the contact angle by using the sessile drop method. The characterization results indicated that silver nanoparticles were formed at a wavelength of 406.60 nm, with their particle size were 200.1 nm. The results of the antimicrobial test showed that modified goat leather using two methods of preparation had a different significance to inhibit the S. epidermidis and E. coli, and also fungi of C. albicans. The leather, after modification with nanoparticle via in situ method, had the highest antibacterial activities against S. epidermidis and E. coli. However, leather after modification with adding nanoparticle and MTMS via ex situ method has the highest antifungal activity against C. albicans. The leather after modification nanoparticle and MTMS via in situ method has the highest tensile strength and the largest toughness. All modified leathers had larger antimicrobial activity, contact angle, and also toughness compared to unmodified leather.

Novel Formulation Development and Evaluation of Nanoparticles Based in Situ Gelling System for The Ophthalmic Delivery of Ciprofloxacin Hydrochloride

2015 ◽  
Vol 5 (4) ◽  
Author(s):  
Kranti Singh ◽  
Surajpal Verma ◽  
Shyam Prasad ◽  
Indu Bala
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Drug Loading ◽  
In Vitro Release ◽  
Formulation Development ◽  
Ciprofloxacin Hydrochloride ◽  
Potential Value ◽  
The Mean ◽  
In Situ Gelling

Ciprofloxacin hydrochloride loaded Eudragit RS100 nanoparticles were prepared by using w/o/w emulsification (multiple emulsification) solvent evaporation followed by drying of nanoparticles at 50°C. The nanoparticles were further incorporated into the pH-triggered in situ gel forming system which was prepared using Carbopol 940 in combination with HPMC as viscosifying agent. The developed nanoparticles was evaluated for particle size, zeta potential value and loading efficiency; nanoparticle incorporated in situ gelling system was evaluated for pH, clarity, gelling strength, rheological studies, in-vitro release studies and ex-vivo precorneal permeation studies. The nanopaticle showed the mean particle size varying between 263.5nm - 325.9 nm with the mean zeta potential value of -5.91 mV to -8.13 mV and drug loading capacity varied individually between 72.50% to 98.70% w/w. The formulation was clear with no suspended particles, showed good gelling properties. The gelling was quick and remained for longer time period. The developed formulation was therapeutically efficacious, stable and non-irritant. It provided the sustained release of drug over a period of 8-10 hours.

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