Emulsijos yra patrauklios išvaizdos, universalūs produktai, jų naudojimas yra paprastas bei priimtinas, dėl to jos yra ypač dažnai sutinkamos dermatologijoje, gydant įvairias odos ligas. Stabilus puskietis emulsinis pagrindas iš natūralių medžiagų yra aktualus, nes turi dideles pritaikymo galimybes kosmetinių ir gydomųjų kremų gamyboje. Tyrimo objektas – puskietė emulsinė sistema vanduo aliejuje iš natūralių medžiagų su bičių vašku, kaip vaistinių medžiagų nešiklis dermatologiniams preparatams. Darbo tikslas – puskietės emulsinės sistemos vanduo aliejuje (v/a) su bičių vašku sumodeliavimas ir modelinės medžiagos – askorbo rūgšties atpalaidavimo iš sumodeliuotos sistemos įvertinimas biofarmaciniu in vitro tyrimu. Tyrimo uždaviniai: parinkti puskietės emulsinės sistemos sudėtį, remiantis ortogonaliu statistiniu planu, ir atrinkti stabilius pavyzdžius pagal pasirinktus vertinimo kriterijus (tinkamas pH, klampa, mikrostruktūra bei juslinės savybės); nustatyti puskiečių emulsinių sistemų fizikocheminius rodiklius (pH, klampą, mikrostruktūrą) bei įvertinti jų stabilumą po 1 ir 3 mėn.; įvertinti bičių vaško įtaką puskiečių emulsinių sistemų klampai, stabilumui, juslinėms savybėms bei askorbo rūgšties atpalaidavimui iš puskietės emulsinės sistemos; įvertinti modelinės medžiagos – askorbo rūgšties atpalaidavimą iš tiriamų puskiečių emulsinių sistemų, atliekant biofarmacinį tyrimą in vitro per pusiau pralaidžią membraną; atlikti emulsinės sistemos juslinių savybių ir kokybės... [toliau žr. visą tekstą] / Emulsion has an attractive conformation and is an universal product. It‘s usage is simple and acceptable. For this reason, it is often used in dermatology for curing different skin disease. Stable semisolid emulsion base from natural materials is relevant because it has a big variety of use in cosmetic and remedial cream production. The object of research – the system of semisolid emulsion water in oil from natural materials and beeswax as a carrier of medical materials in dermatological preparations. The aim of the work – modeling the system of semisolid emulsion water in oil with the beeswax and modeling materials as liberation ascorbic acid from simulated system and it‘s biopharmacy evaluation by in vitro research. The task of research: to choose the composition of semisolid emulsion system on the ground of orthogonal statistic plan and select stable samples according to evaluation criterion (the proper pH, viscosity, microstructure and organoleptic properties); to rate physicochemical rates of the system of semisolid emulsion (pH, viscosity, microstructure) and evaluate their stability after 1 and 3 months; to evaluate the influence of beeswax on the viscosity, stability, sensual properties and the liberation of ascorbic acid from the system of semisolid emulsion; to evaluate modeling materials – the liberation of ascorbic acid from investigative system of semisolid emulsion carrying out biopharmacy research in vitro through semi-permeable membrane; to evaluate sensual... [to full text]

Magister Pharmaceuticae - MPharm / Background: Tenofovir disoproxil fumarate (TDF) and Zidovudine (AZT) are both nucleotide and nucleoside analogue reverse transcriptase inhibitors (NtRTIs and NRTIs), respectively. They are used for the management and prevention of the Human Immunodeficiency Virus (HIV) infection. These drugs are faced with oral delivery challenges such as low intestinal permeability and extensive first pass liver metabolism for TDF and AZT, respectively. Their use may also be limited by dose-dependent adverse effects, which may result in treatment failure when patients become non-compliant and non-adherent to their prescribed antiretroviral (ARV) regimen. Non-compliance and non-adherence to ARV regimen may lead to drug resistance and a need for change in regimen, which can be very expensive, not only financially but in terms of morbidity and mortality. To solve such issues, a new drug can be formulated, or an existing drug can be modified. The development and formulation of a new drug is time consuming and expensive, especially with no available data and a high probability of failure. Modifying existing drugs is a cheaper, less time-consuming option with lower probability of failure. Such modification can be achieved via non-covalent interactions using various methods such as preparation of nano-particulates with polymeric micelles (a non-covalent interaction). Polymeric micelles offer a variety of polymers to choose from for drug modification purposes. Purpose: The aim of this study was to formulate polymeric nanoparticles of TDF and AZT using different ratios of poly-lactic-co-glycolic acid (PLGA), characterize the formulated nanoparticles (using the following analyses: particle size, zeta potential, encapsulation efficiency, hot stage microscopy, thermogravimetric analysis, differential scanning calorimetry, Fourier transform infrared spectroscopy and scanning electron microscopy), analyze for stability during storage (2-8˚C) and determine the release rate of the active pharmaceutical ingredients in the formulated nanoparticles. Methods: Nanoparticles were prepared using a modified version of the double emulsion (water-in-oil-in-water) solvent evaporation and diffusion method. Two ratios of PLGA (50:50 and 85:15) were used to prepare four formulations (two each of TDF and AZT). Thereafter, the physicochemical and pharmaceutical properties of the formulations were assessed by characterizing the nanoparticles for particle size, zeta potential, polydispersity index, percentage yield, release profile and particle morphology, using the suggested analytical techniques. Results: For TDF-PLGA 85:15, TDF-PLGA 50:50, AZT-PLGA 85:15 and AZT-PLGA 50:50, nanoparticles of 160.4±1.7 nm,154.3±3.1 nm,127.0±2.32 nm and 153.2±4.3 nm, respectively, were recovered after washing. The polydispersity index (PDI) values were ≤0.418±0.004 after washing, indicating that the formulations were monodispersed. The zeta potential of the particles was -5.72±1 mV, -19.1 mV, -12.2±0.6 mV and -15.3±0.5 mV for TDF-PLGA 85:15, TDF-PLGA 50:50, AZT-PLGA 85:15 and AZT-PLGA 50:50 respectively after washing. The highest percentage yield was calculated to be 79.14% and the highest encapsulation efficiency obtained was 73.82% for AZT-PLGA 50:50, while the particle morphology showed spherical nanoparticles with signs of coalescence and aggregation for all formulated nanoparticles. The release profiles were biphasic; that is, an initial burst which indicated the presence of surface API followed by sustained release. Comparing the release profiles of AZT and TDF at pH 1.2 and 7.4, it was indicative that more AZT was released at pH 1.2 while more TDF was released at pH 7.4. On computing the release data further into various mathematical models, the Weibull model was found to be the best fit. The loaded nanoparticles showed an increase in stability after washing; however, they showed signs of gradual decrease in stability after 10 days of storage at 2-8°C. Conclusions: Relatively small, spherical and smooth nanoparticles were formulated. The nanoparticle release profile was indicative of sustained release; however, there was no conclusive indication that 48 hours duration was sufficient to release all encapsulated drug. Further studies with an increased API or polymer ratio in the formulation needs to be performed to determine if the encapsulation efficiency can be improved and in-vivo studies are required for a better understanding of the API release from formulations as well as its absorption in the body.