There has been growing interest in designing and development of suitable micro or nano drug delivery system with the ability to target site specifically and release the payload in a predetermined fashion. Recently a new type of system called polyelectrolyte microcapsules and thin films have been proposed and developed for applications such as, biomedical devices to micro sensing and drug delivery. Owing to its advantages of mild preparation conditions, multifunctionality, with programmable characteristics and to encapsulate large amount of materials, it has shown immense potential. In the present research, multilayer polyelectrolyte thin films composed of Poly(methacrylic acid) (PMA) and Poly (vinyl pyrrolidone) (PVP) were deposited on the flat substrates using layer by layer (LBL) technique. The film growth and its deconstruction under physiological conditions were characterized using UV Visible spectrophotometer and Scanning Electron Microscopy (SEM). Hollow microcapsules composed of PMA and PVP were also produced with the help of sacrificial silica template using the same LBL adsorption technique. After coating the desired number of PVP and PMA layers, the colloidal template was removed with a buffer system composed of Hydrofluoric acid (HF) and Ammonium fluoride (NH4F). The obtained capsules were characterized for its surface morphology using SEM and Atomic Force Microscopy (AFM). The hydrogen bonding in capsule formation was confirmed by Fourier Transform Infrared Spectroscopy (FTIR). Encapsulation and release with the microcapsules was carried out using Rifampicin (Antitubercular drug) as a model drug. The interaction of empty and drug loaded capsules with Mycobacterium Smegmatis cell line was investigated. It was found that the empty capsules did not affect the cell growth indicating their biocompatibility. Confocal microscopy studies with Doxorubicin (anticancer drug), which is a naturally fluorescent molecule, showed the drug is indeed encapsulated inside the hollow capsule. From the above studies, it was concluded that polyelectrolyte capsules have the potential to be used for delivering drugs.

Cápsulas gelatinosas são formas farmacêuticas empregadas para a veiculação de fármacos por via oral. Há diversas vantagens em sua utilização como a facilidade de deglutição, mascaramento do sabor e odor de fármacos e rápida disponibilização de seu conteúdo no trato gastrointestinal. Atualmente, as cápsulas são as principais formas farmacêuticas nos estabelecimentos magistrais. Como formas de liberação imediata, seu comportamento após a deglutição deve permitir a rápida liberação do(s) fármaco(s). Desta forma, fatores como a escolha correta de excipientes, observando-se a compatibilidade entre estes e o fármaco, deve ser baseada nas características físico-químicas de ambos para a obtenção de um produto eficaz. As etapas de preparo não são menos relevantes e merecem atenção, como a pesagem, a mistura e o enchimento. O objetivo deste trabalho foi discutir o tema cápsulas, salientando fatores acerca de seu emprego como forma farmacêutica, elaboração de formulações, produção e controle, visando a adequada aplicabilidade no setor magistral. / Gelatin capsules are pharmaceutical forms employed in oral drug delivery. There are many advantages on its use like easy deglutition, smell and tast masking and fast availability of its content in gastrointestinal tract. Nowadays, the capsules are the main drug delivery forms used on magistral pharmacies. As immediate drug delivery forms its behavior after deglutition should promote a fast availability of the drug(s). Thus, the right choice of the excipients, observing the compatibility between these and the drug, should be based on physicochemical caracteristhics of the compounds to achieve an adequate product. The production steps are not less relevant and deserve an appropriate attention, Iike weighing, mixture and filling. The goal of this work was discussing the theme capsules, exploring factors around its employing as drug delivery form, formulations development, production and control, seeking a suitable applicability on magistral field.

This thesis investigates the transport and sorting of capsules (elastic membranes enclosing a liquid core) using viscous flow in complex vessel geometries. Of particular interest is passive sorting by deformability using only the fluid-structure interaction between the capsule, the viscous fluid and the geometry of the vessel. Millimetric alginate-ovalbumin capsules in the regime of negligible fluid inertia are used in this work. In order to characterise the elastic properties of the capsules, a novel numerical finite element model of the compression of a thick-shelled capsule between parallel plates is implemented. The constitutive model of the capsule membranes was determined by comparison to experimental data: a Yeoh constitutive model with the ratio of constants $C_1 = 1$, $C_2 = 0$ and $C_3 = 10$ describes the capsules used. Three geometries are investigated in this work. (i) A T-Junction bifurcation. Capsule deformation in the T-Junction bifurcation is characterised by the maximal length of the capsule $L_{max}$ and depends on the ratio of viscous to elastic forces, the capillary number $Ca$. The maximal length, $L_{max}$, is especially sensitive at distinguishing soft capsules by their deformability. The sensitivity of $L_{max}$ to capsule compliance and the large deformations that can be achieved makes the T-junction a promising geometry in which to measure elastic properties of the capsules. The rate of relaxation of the capsules after the bifurcation is independent of their deformation. (ii) A half-cylinder obstacle in a channel followed by a sudden expansion. We show that the half-cylinder obstacle causes capsule trajectories to vary depending on deformability. Capsules with a factor of three difference in deformability can be separated. A practical feature of the system is its relative insensitivity to the initial lateral position of the capsules in the channel. However, while the results are reproducible across different capsules, the variations in final position amount to 10 \% at fixed parameters. As these experiments were conducted with the same capsule under identical flow conditions, this is likely to represent the best case scenario. (iii) We adapt the pinched flow fractionation (PFF) geometry to the sorting of capsules. We show that the standard PFF device cannot be used to sort capsules. However, a novel mode of operation, termed the ``T-Junction'' mode, shows great promise for the sorting of capsules. The PFF device in the T-Junction mode separates capsules with a factor of 1.5 difference in deformability. This is twice as sensitive as the half-cylinder device, although larger variability was observed in the PFF device.

This dissertation describes the effective encapsulation of redox active compounds inside deep-cavity cavitands: Gibb's octaacid40 and Rebek's 41 tetracarboxylate cavitand. Gibb's octaacid is a water-soluble, deep-cavity cavitand that forms well-characterized dimeric molecular capsules around hydrophobic guests. Both 1H NMR spectroscopic and voltammetric experiments clearly reveal that ferrocene plays the role of hydrophobic guest effectively. Ferrocene derivatives (ferrocenylmethyltrimethylammonium (FcNMe3+), ferrocenemethanol (FcOH), and ferrocene carboxylic acid (FcCOOH)) were also found to form inclusion complexes with octaacid cavitand however, in this case 1:1 (host to guest) ratio complexes are formed. This is in strong contrast with the dimeric capsule formed around ferrocene. Under the surveyed experimental conditions encapsulated ferrocene is electrochemically silent. We have also found that the negative charges around this dimeric molecular capsule play a very important role. For instance, hydrophobic cations, such as viologens,60 bind to the outer surface of the capsule. This opened a possibility of mediated electron transfer reactions between molecules bound inside the octaacid capsule and tightly attached to its outer surface in purely synthetic system. The cationic ferrocene derivative, ferrocenylmethyltrimethylammonium (FcNMe3+), was used as a mediator since its electrochemical potential range makes it suitable as a mediator molecule. In fact, our data clearly support that FcNMe3+ mediates electron transfer between encapsulated ferrocene and the electrode surface. Ferrocene, its derivatives (FcNMe3+ and FcOH), and cobaltocenium (Cob+) also form 1:1 inclusion complexes with Rebek's tetracarboxylate cavitand, which surprisingly are all voltammetrically silent. The formation of these inclusion complexes seems to be driven by hydrophobic interactions between the host and the guest. The lack of voltammetric response observed in this work is a very intriguing finding.

Self-organization is a common occurrence among molecules in nature and questions of how and why these molecules interact and come together by intermolecular forces has been under investigation by those interested in molecular recognition. Synthetic molecules able to mimic nature have become important in the area of supramolecular chemistry. Calixarenes are a group of molecules that is being investigated for their ability to self-assemble into dimeric capsules. Such capsules can be very useful for catalysis, molecular recognition and for encapsulation. The synthetic stratergies involved in the synthesis of a diureidocalix[4]arene is presented. In this case the taget molecule is a tetrapropylcalix[4]arene substituted on the upper rim with two urea groups separated by a hydrocarbon chain will be synthesized. This molecule can then be used to investigate its dimerization properties.

Thesis (Ph.D.)--University of Alabama at Birmingham, 2009. / Title from PDF title page (viewed on Feb. 2, 2010). Includes bibliographical references (p. 64-72).

Renal failure uremia occurs when the kidneys fail to function properly. Despite being the main treatment, dialysis and other therapeutic approaches are not only associated with numerous long-term adverse complications often leading to morbidity and mortality events, but are also not affordable. Orally administrating Alginate-Poly-L-Lysine-Alginate microcapsules entrapping live yeast cells to treat renal failure uremia has not yet been investigated. In this thesis, the growth and microencapsulation of yeast were optimized. The efficacy of these microcapsules in removing unwanted electrolytes was tested in vitro in simulated gastro-intestinal media, in vitro in a column bioreactor and in vivo in an uremic rat model. Results showed that these novel microcapsules can not only maintain morphological stability and membrane integrity under gastro-intestinal environments and mechanical stresses, but also, preserve the viability of yeast. These microcapsules were successful in reducing urea concentrations while not harming the human GI tract's microbial flora.

Diss. (sammanfattning) Stockholm : Karol. inst., 2002. / Härtill 4 uppsatser.

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