Control of molecular polymorphisms by a structured carbohydrate / ceramic delivery vehicle — aquasomes

• Published in: Journal of controlled release Vol. 39; no. 2; pp. 383 - 388
• Main Authors: Kossovsky, N., Gelman, A., Rajguru, S., Nguyen, R., Sponsler, E., Hnatyszyn, H.J., Chow, K., Chung, A., Torres, M., Zemanovich, J., Crowder, J., Bamajian, P., Ly, K., Philipose, J., Ammons, D., Anderson, S., Goodwin, C., Soliemanzadeh, P., Yao, G., Wei, K
• Format: Journal Article Conference Proceeding
• Language: English
• Published: Amsterdam Elsevier B.V 01.05.1996; Elsevier
• Subjects: Biological and medical sciences; Carbohydrate; Ceramic; Denaturation; Drug delivery; General pharmacology; Medical sciences; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Surface; Ceramic; Carbohydrate; Drug delivery; Denaturation; Surface; Drug; Delivery system; Pharmaceutical technology; Intravenous administration; Peptides; Physical properties; Biological activity; Antigen; Prevention; Stabilizer agent; Animal; Dosage form; Hemoglobin; Ceramic materials
• ISSN: 0168-3659; 1873-4995
• DOI: 10.1016/0168-3659(95)00169-7

Molecular denaturation of polypeptides and other macromolecular pharmaceuticals upon surface adsorption from an aqueous environment is almost inevitable. Molecular denaturation, coupled with a net increase in entropy, accounts for the net negative ΔG and frequent irreversible nature of surface adsorption. The consequence of this interaction is that surface immobilized drugs lose their dynamic freedom and thus, all too often, their biological activity. A drug delivery system based on a novel surface modification process to help reverse the constraining activity of surfaces is described. Beginning with preformed carbon ceramic nanoparticles and self-assembled calcium-phosphate dihydrate particles (colloidal precipitation) to which glassy carbohydrates are then allowed to adsorb as a nanometer thick surface coating, a molecular carrier is formed. The carbohydrate coating functions as a dehydroprotectant and stabilizes subsequently non-covalently bound immobilized members of biochemically reactive surface members such as pharmaceuticals. Many of the physical properties of this enabling system have been characterized in vitro and in animal models. Antigen delivery, drug delivery, and hemoglobin delivery experiments are described.