Abstract
The aim of this work was to evaluate unilamellar liposomes as new potential capreomycin sulfate (CS) delivery systems for future pulmonary targeting by aerosol administration. Dipalmitoylphosphatidylcholine, hydrogenated phosphatidylcholine, and distearoylphosphatidylcholine were used for liposome preparation. Peptide-membrane interaction was investigated by differential scanning calorimetry (DSC) and attenuated total internal reflection Fourier-transform infrared spectroscopy (ATIR-FTIR). Peptide entrapment, size, and morphology were evaluated by UV spectrophotometry, photocorrelation spectroscopy, and transmission electron microscopy, respectively. Interaction between CS and the outer region of the bilayer was revealed by DSC and ATIR-FTIR. DSPC liposomes showed enhanced interdigitation when the CS molar fraction was increased. Formation of a second phase on the bilayer surface was observed. From kinetic and permeability studies, CS loaded DSPC liposomes resulted more stable if compared to DPPC and HPC over the period of time investigated. The amount of entrapped peptide oscillated between 10% and 13%. Vesicles showed a narrow size distribution, from 138 to 166 nm, and a good morphology. These systems, in particular DSPC liposomes, could represent promising carriers for this peptide.
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References
Maher D, Floyd K, Raviglione M. A strategic framework to decrease the burden of TB/HIV. WHO report, World Health Organization/ Communicable Disease/Tuberculosis, 2002; 296.
Vigorita MG, Ottana R, Zappalà C, Maccari R, Pizzimenti FC, Gabrielli G. Halogenated isoniazid derivatives as possible antimy cobacterial and anti-HIV agents-III.IL Farmaco. 1994;49:775–781.
Ferrarini P, Manera C, Mori C, Badawneh M, Saccomanni G. Synthesis and evaluation of antimycobacterial activity of 4-phenyl-1,8-naphthyridine derivatives.II Farmaco. 1999;53:741–746.
Gursoy A. Liposome-encapsulated antibiotics: Physicochemical and antibacterial properties, a review.STP Pharma Sci. 2000;10(4):285–291.
Deol P, Khuller GK. Lung specific stealth liposomes: stability, biodistribution and toxicity of liposomal antitubercular drugs in mice.Biochim Biophys Acta 1997;1334:161–172.
Pinto-Alphandary H, Andremont A, Couvreur P. Targeted delivery antibiotics using liposomes and nanoparticles: research and applications.Int J Antimicrob Agents. 2000;13:155–168.
Le Conte P, Le Gallou F, Potel G, Struillou L, Baron D, Drugeon HB. Pharmacokinetics, toxicity, and efficacy of liposomal capreomycin in disseminatedMycobacterium avium beige mouse model.Antimicrob Agents Chemother. 1994;38:2695–2701.
Martindale the Extra Pharmacopoeia. Capreomycin sulfate (7554-1).The Complete Drug Reference—Monographs. 3 2nd ed. Parfitt K editor, The Pharmaceutical Press, London, UK; 1997:162.
Fattorini L, Iona E, Ricci ML, Thoresen OF, Orru G, Oggioni MR, Tortoli E, Piersimoni C, Chiaradonna P, Tronci M, Pozzi G, Orefici G. Activity of 16 antimicrobial agents against drug-resistant strains of Mycobacterium tuberculosis.Microb Drug Resist. 1999;5:265–270.
Farr SJ, Kellaway IW, Perry-Jones DR, Woolfrey SG. 99-m Technetium as a marker of liposomal deposition and clearance in the human lung.Int J Pharm. 1985;26:303–316.
Gilbert BE, Six HR, Wilson SZ, Wyde PR, Knight V. Small particle aerosols of enviroxime-containing liposomes.J Antiviral Res. 1988;9:355–365.
Niven RW, Schreier H. Nebulization of liposomes, I: effects of lipid composition.Pharm Res. 1990;7:1127–1133.
Schreier H, Gonzalez-Rothi RJ, Steceko AA. Pulmonary delivery of liposomes.J Control Release. 1993;24:209–223.
Taylor KMG, Farr SJ. Liposomes for delivery to the respiratory tract.Drug Dev Ind Pharm. 1993;19:123–142.
Hung OR, Whynot SC, Varnel JR, Shafer SL, Mezel M. Pharmacokinetics of inhaled liposome encapsulated fentanyl.Anesthesiology. 1995;83:277–284.
Patton JS, Platz RM. Pulmonary delivery of peptides and proteins for systemic action.Adv Drug Deliv Rev. 1992;8:179–196.
Niven RW, Speer M, Schreier H. Nebulization of liposomes, II: the effects of size and modelling of solute release profiles.Pharm Res. 1991;8:2 217–221.
Mayer LD, Hope MJ, Cullis PR. Vesicles of variable, sizes produced by a rapid extrusion procedure.Biochim Biophys Acta. 1986:858:161–168.
Sivakuma PA, Panduranga KR. Development of stable polymerized vinyl-pyrrolidone cholesteryl methacrylate liposomes as carriers for drug delivery.Biomed Microdev. 2002;4:3, 197–204.
Moscho A, Orwar O, Chiu DT, Modi BP, Zare RN. Rapid preparation of giant unilamellar vesicles.Proc Natl Acad Sci USA. 1996;93:11443–11447.
Goormaghtigh E, Raussens V, Ruysschaert JM. Attenuated total reflection infrared spectroscopy of proteins and lipids in biological membranes.Biochim Biophys Acta 1999;1422:105–185.
Jain MK. Order and dynamics in bilayers and solute in bilayers. In: Jain MK, ed.Introduction to Biological Membranes. New York, NY: Wiley, 1988:122–165.
Taylor KMG, Morris RM. Thermal analysis of phase transition behaviour in liposomes.Thermochim Acta. 1995;248:289–301.
Weers JG, Scheuing DR. Characterization of viscoelatic surfactant mixtures, I: Fourier transform infrared spectroscopic studies.Colloids Surf. B: Biointerfaces, 1991;55:41–56.
Fringeli UP, Guenthard HH. Infrared membrane spectroscopy.Mol Biol Biochem Biophys. 1981;31:270–332.
Guenzler H, Boeck H.IR Spectroscopy. An Introduction. 2nd ed. Weinheim, Germany: Verlag Chemie, 1983:403. (In German).
Silvestro L, Axelsen PH. Infrared spectroscopy of supported lipid monolayer, bilayer, multibilayer membranes.Chem Phys Lipids. 1998;96:69–80.
Attar M, Wong PTT, Kates M, Carrier D, Jaklis P, Tanphaichitr N. Interaction between sulfogalactosylceramide and dimyristoylphosphatidylcholine increases the orientational fluctuation of their lipid hydrocarbon chains.Chem Phys, Lipids. 1998;94:227–238.
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Giovagnoli, S., Blasi, P., Vescovi, C. et al. Unilamellar vesicles as potential capreomycin sulfate carriers: Preparation and physicochemical characterization. AAPS PharmSciTech 4, 69 (2003). https://doi.org/10.1208/pt040469
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DOI: https://doi.org/10.1208/pt040469