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Native hyaluronan as a delivery system for hydrophobic drugs
Černá, Eva ; Mravec, Filip (referee) ; Pekař, Miloslav (advisor)
The aim of this paper is to discover whether it is possible to use the native form of hyaluronic acid as a hydrophobic drug carrier for a targeted distribution in the body. In its structure, hyaluronic acid is a linear high molecular weight biopolysaccharide which is found in most living organisms. Hyaluronan is involved in many physiological processes and therefore is essential for the functionality of the human body. It is in most tissues of the human body, high concentration is in the skin, the vitreous body and is also observed in cancer cells that contain several receptors for hyaluronan. These receptors include CD44 and RHAMM. The interaction of the hyaluronic acid delivery system and the hydrophobic medicinal with these receptors could ensure a free passage for drugs to the affected tissue, where the release of the drug would destroy the affected cells. The drug would directly target the damaged tissue and did not burden the rest of the body like the cytotoxic agents do. In this paper the native form of hyaluronic acid, which we normally find in the human organism, was chosen as the carrier. Its properties do not stand above other carrier systems, but its biocompatibility and biodegradability in the body greatly exceed them. High molecular weight hyaluronic acid was used as a carrier and the hydrophobic dye sudan red G, a substance of similar properties, was used instead of a hydrophobic drug.
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The study of polymorphism and optimization of active pharmaceutical ingredients crystallisation
Novák, David ; Ing.Ladislav Cvak, Ph.D. (referee) ; Ing.Roman Gabriel (advisor)
Active pharmaceutical ingredients (APIs) are frequently delivered to the patient in the solid-state as part of an approved dosage form (tablets, capsules, etc.). Understanding and controlling the solid-state chemistry of APIs is therefore an important aspect of the drug development process. APIs can exist in a variety of distinct solid forms, including polymorphs, solvates, hydrates, co-crystals and amorphous solids. Each form displays unique physicochemical properties that can profoundly influence the bioavailability, manufacturability, stability and other performance characteristics of the drug. Most APIs are purified and isolated by crystallisation from an appropriate solvent during the final step in synthetic process. The main objective of a crystallisation process is to produce crystals with desired properties such as particle size distribution (PSD), shape and purity. All pharmaceutical dosage forms must be produced in uniform units, and good content of uniformity is only possible when the size of the active component is carefully controlled. For on-line control of crystallisations of Quetiapine Fumarate to achieve desired PSD and no changed physicochemical purity was used the Lasentec Focus Beam Reflectance Measurement (FBRM) system.
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Influence of formulation factors on the characteristics of terbinafine loaded nanoparticles.
Barák, Vlastimil ; Šnejdrová, Eva (advisor) ; Dittrich, Milan (referee)
CHARLES UNIVERSITY FACULTY OF PHARMACY IN HRADEC KRÁLOVÉ DEPARTMENT OF PHARMACEUTICAL TECHNOLOGY Author: Vlastimil Barák Title of Diploma thesis The influence of formulation factors on the characteristics of terbinafine loaded nanoparticles Supervisor: PharmDr. Eva Šnejdrová, Ph.D. Consultant: Mgr. Juraj Martiška The diploma thesis is focused on biodegradable polymer nanoparticles loaded by terbinafine based on the copolymer of glycolic and lactic acid branched on polyacrylic acid. The nanoprecipitation method was employed, and the influence of formulation factors on nanoparticle characteristics was studied. The following formulation factors were the concentration of the polymer, the amount of terbinafine, and the concentration of surfactant. Nanoparticles of 120 nm to 300 nm were obtained depending on the preparation conditions. The nanoparticle polydispersity was in all cases from 0.080 to 0.230. The prepared nanoparticles were stable, as evidenced by zeta potential values above 38 mV. A positive zeta potential is desirable for dermal and mucosal adhesion in the topical and ocular application of nanoparticles with terbinafine. The amount of polymer used to form nanoparticles has the greatest effect on particle size. With increasing polyester concentration in the internal phase, the size of the...
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Terbinafine-loaded biodegradable polymeric systems for topical administration
Pokorná, Tereza ; Šnejdrová, Eva (advisor) ; Dittrich, Milan (referee)
CHARLES UNIVERSITY FACULTY OF PHARMACY IN HRADEC KRÁLOVÉ DEPARTMENT OF PHARMACEUTICAL TECHNOLOGY Author: Tereza Pokorná Title of Diploma thesis Terbinafine-loaded biodegradable polymeric systems for topical administration Supervisor: PharmDr. Eva Šnejdrová, Ph.D. In the diploma thesis the released properties of solid dispersions with terbinafine, based on polyesters of D,L-lactic acid and glycol acid, branched with pentaerythritol and tripentaerythritol are studied. The theoretical part deals with solid dispersions, their classification and methods of preparation, methods of drug dissolution testing, properties, effect, use of terbinafine and preparations containing terbinafine. In the experimental part, solid dispersions were prepared by the melting method. The drug was incorporated into the polyester in the form of a hydrochloride or a base in a concentration of 10 % or 20 %. Some systems were plasticized with 30% triethyl citrate. Thin layers were formulated from solid dispersions, and drug dissolution tests were performed on phosphate buffer pH 7.4 at 37 řC. Assay of terbinafine released was performed spectrophotometrically at 223 nm and ultra-high performance liquid chromatography. Based on the results of this diploma thesis, it can be clearly stated that the suitable carrier of terbinafine...
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Influence of formulation factors on the characteristics of terbinafine loaded nanoparticles.
Barák, Vlastimil ; Šnejdrová, Eva (advisor) ; Dittrich, Milan (referee)
CHARLES UNIVERSITY FACULTY OF PHARMACY IN HRADEC KRÁLOVÉ DEPARTMENT OF PHARMACEUTICAL TECHNOLOGY Author: Vlastimil Barák Title of Diploma thesis The influence of formulation factors on the characteristics of terbinafine loaded nanoparticles Supervisor: PharmDr. Eva Šnejdrová, Ph.D. Consultant: Mgr. Juraj Martiška The diploma thesis is focused on biodegradable polymer nanoparticles loaded by terbinafine based on the copolymer of glycolic and lactic acid branched on polyacrylic acid. The nanoprecipitation method was employed, and the influence of formulation factors on nanoparticle characteristics was studied. The following formulation factors were the concentration of the polymer, the amount of terbinafine, and the concentration of surfactant. Nanoparticles of 120 nm to 300 nm were obtained depending on the preparation conditions. The nanoparticle polydispersity was in all cases from 0.080 to 0.230. The prepared nanoparticles were stable, as evidenced by zeta potential values above 38 mV. A positive zeta potential is desirable for dermal and mucosal adhesion in the topical and ocular application of nanoparticles with terbinafine. The amount of polymer used to form nanoparticles has the greatest effect on particle size. With increasing polyester concentration in the internal phase, the size of the...
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Influence of formulation factors on the characteristics of terbinafine loaded nanoparticles.
Barák, Vlastimil ; Šnejdrová, Eva (advisor) ; Dittrich, Milan (referee)
CHARLES UNIVERSITY FACULTY OF PHARMACY IN HRADEC KRÁLOVÉ DEPARTMENT OF PHARMACEUTICAL TECHNOLOGY Author: Vlastimil Barák Title of Diploma thesis The influence of formulation factors on the characteristics of terbinafine loaded nanoparticles Supervisor: PharmDr. Eva Šnejdrová, Ph.D. Consultant: Mgr. Juraj Martiška The diploma thesis is focused on biodegradable polymer nanoparticles loaded by terbinafine based on the copolymer of glycolic and lactic acid branched on polyacrylic acid. The nanoprecipitation method was employed, and the influence of formulation factors on nanoparticle characteristics was studied. The following formulation factors were the concentration of the polymer, the amount of terbinafine, and the concentration of surfactant. Nanoparticles of 120 nm to 300 nm were obtained depending on the preparation conditions. The nanoparticle polydispersity was in all cases from 0.080 to 0.230. The prepared nanoparticles were stable, as evidenced by zeta potential values above 38 mV. A positive zeta potential is desirable for dermal and mucosal adhesion in the topical and ocular application of nanoparticles with terbinafine. The amount of polymer used to form nanoparticles has the greatest effect on particle size. With increasing polyester concentration in the internal phase, the size of the...
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Influence of formulation factors on the characteristics of terbinafine loaded nanoparticles.
Barák, Vlastimil ; Šnejdrová, Eva (advisor) ; Dittrich, Milan (referee)
CHARLES UNIVERSITY FACULTY OF PHARMACY IN HRADEC KRÁLOVÉ DEPARTMENT OF PHARMACEUTICAL TECHNOLOGY Author: Vlastimil Barák Title of Diploma thesis The influence of formulation factors on the characteristics of terbinafine loaded nanoparticles Supervisor: PharmDr. Eva Šnejdrová, Ph.D. Consultant: Mgr. Juraj Martiška The diploma thesis is focused on biodegradable polymer nanoparticles loaded by terbinafine based on the copolymer of glycolic and lactic acid branched on polyacrylic acid. The nanoprecipitation method was employed, and the influence of formulation factors on nanoparticle characteristics was studied. The following formulation factors were the concentration of the polymer, the amount of terbinafine, and the concentration of surfactant. Nanoparticles of 120 nm to 300 nm were obtained depending on the preparation conditions. The nanoparticle polydispersity was in all cases from 0.080 to 0.230. The prepared nanoparticles were stable, as evidenced by zeta potential values above 38 mV. A positive zeta potential is desirable for dermal and mucosal adhesion in the topical and ocular application of nanoparticles with terbinafine. The amount of polymer used to form nanoparticles has the greatest effect on particle size. With increasing polyester concentration in the internal phase, the size of the...
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Terbinafine-loaded biodegradable polymeric systems for topical administration
Pokorná, Tereza ; Šnejdrová, Eva (advisor) ; Dittrich, Milan (referee)
CHARLES UNIVERSITY FACULTY OF PHARMACY IN HRADEC KRÁLOVÉ DEPARTMENT OF PHARMACEUTICAL TECHNOLOGY Author: Tereza Pokorná Title of Diploma thesis Terbinafine-loaded biodegradable polymeric systems for topical administration Supervisor: PharmDr. Eva Šnejdrová, Ph.D. In the diploma thesis the released properties of solid dispersions with terbinafine, based on polyesters of D,L-lactic acid and glycol acid, branched with pentaerythritol and tripentaerythritol are studied. The theoretical part deals with solid dispersions, their classification and methods of preparation, methods of drug dissolution testing, properties, effect, use of terbinafine and preparations containing terbinafine. In the experimental part, solid dispersions were prepared by the melting method. The drug was incorporated into the polyester in the form of a hydrochloride or a base in a concentration of 10 % or 20 %. Some systems were plasticized with 30% triethyl citrate. Thin layers were formulated from solid dispersions, and drug dissolution tests were performed on phosphate buffer pH 7.4 at 37 řC. Assay of terbinafine released was performed spectrophotometrically at 223 nm and ultra-high performance liquid chromatography. Based on the results of this diploma thesis, it can be clearly stated that the suitable carrier of terbinafine...
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Terbinafine-loaded biodegradable polymeric systems for topical administration
Pokorná, Tereza ; Šnejdrová, Eva (advisor) ; Dittrich, Milan (referee)
CHARLES UNIVERSITY FACULTY OF PHARMACY IN HRADEC KRÁLOVÉ DEPARTMENT OF PHARMACEUTICAL TECHNOLOGY Author: Tereza Pokorná Title of Diploma thesis Terbinafine-loaded biodegradable polymeric systems for topical administration Supervisor: PharmDr. Eva Šnejdrová, Ph.D. In the diploma thesis the released properties of solid dispersions with terbinafine, based on polyesters of D,L-lactic acid and glycol acid, branched with pentaerythritol and tripentaerythritol are studied. The theoretical part deals with solid dispersions, their classification and methods of preparation, methods of drug dissolution testing, properties, effect, use of terbinafine and preparations containing terbinafine. In the experimental part, solid dispersions were prepared by the melting method. The drug was incorporated into the polyester in the form of a hydrochloride or a base in a concentration of 10 % or 20 %. Some systems were plasticized with 30% triethyl citrate. Thin layers were formulated from solid dispersions, and drug dissolution tests were performed on phosphate buffer pH 7.4 at 37 řC. Assay of terbinafine released was performed spectrophotometrically at 223 nm and ultra-high performance liquid chromatography. Based on the results of this diploma thesis, it can be clearly stated that the suitable carrier of terbinafine...
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Native hyaluronan as a delivery system for hydrophobic drugs
Černá, Eva ; Mravec, Filip (referee) ; Pekař, Miloslav (advisor)
The aim of this paper is to discover whether it is possible to use the native form of hyaluronic acid as a hydrophobic drug carrier for a targeted distribution in the body. In its structure, hyaluronic acid is a linear high molecular weight biopolysaccharide which is found in most living organisms. Hyaluronan is involved in many physiological processes and therefore is essential for the functionality of the human body. It is in most tissues of the human body, high concentration is in the skin, the vitreous body and is also observed in cancer cells that contain several receptors for hyaluronan. These receptors include CD44 and RHAMM. The interaction of the hyaluronic acid delivery system and the hydrophobic medicinal with these receptors could ensure a free passage for drugs to the affected tissue, where the release of the drug would destroy the affected cells. The drug would directly target the damaged tissue and did not burden the rest of the body like the cytotoxic agents do. In this paper the native form of hyaluronic acid, which we normally find in the human organism, was chosen as the carrier. Its properties do not stand above other carrier systems, but its biocompatibility and biodegradability in the body greatly exceed them. High molecular weight hyaluronic acid was used as a carrier and the hydrophobic dye sudan red G, a substance of similar properties, was used instead of a hydrophobic drug.
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