Effect of Stabilizers and Process Parameters for Budesonide Loaded PLGANanoparticles
Keywords:
Budesonide, nanoparticles, polyvinylalcohol, carbomer, poloxamer, homogenizationAbstract
The present work is aimed at investigations of the effects of various stabilizers and process parameters on the properties of budesonide (glucocorticoid steroid) loaded PLGA (Poly-dl-lactide-co-glycolide) nanoparticles. Budesonide loaded PLGA nanoparticles were prepared following high pressure emulsification- solvent evaporation technique. The effects of three different stabilizers like polyvinylalcohol (PVA), carbomer (Carbopol 980) and poloxamer (Lutrol F-68) are used during emulsification process were studied. Investigations were also carried out regarding influences of different homogenization parameters (pressure and number of cycles) on the properties of various nanoparticles. For comparison, nanoparticles were prepared without the treatment of high pressure also. Various properties of nanoparticles subjected to investigations include, particle size, polydispersity index, drug loading, encapsulation efficiency and the drug release profile. These properties were found to be strongly influenced by the type of stabilizer, homogenization pressure and the number of cycles. Amongst three stabilizers, PVA found to produce comparatively smallest nanoparticles than poloxamer and carbomer. The nanoparticles prepared without high pressure homogenization found to posse’s larger size and high values of polydispersity index especially with the stabilizers carbomer and poloxamer. The low drug loading of nanoparticles found, could be resulted due to high pressure promoted drug diffusion from the protoparticles during the emulsification process and the characteristics of the outer water phase of emulsion. Faster drug release was observed from the nanoparticles obtained after high pressure emulsification as compared to those prepared without pressure homogenization of emulsion.
References
Coombes AGA, Rafati H, Adler J,
Holland J, Davis SS. Proteinloaded poly
(d, l-lactide –co -glycolide) microparticles
for oral administration: formulation,
structural and release characteristics.
Journal of Controlled Release,
;43:89–102.
Gurny R, Ibrahim H, Aebi A, Buri P,
Wilson CG, Washington N, Edman P,
Camber O. Design and evaluation of
controlled release system for the eye.
Journal of Controlled Release,
;6:367–373.
Tice TR, Mason DW, Gilley RM,.
Clinical use and future of parenteral
microsphere delivery systems. In Novel
Drug Delivery, edited by G. F. Prescott
and W. S. Nimmo (Chichester: Wiley),
;24:223–235.
Bodmeier R, McGinity JW. The
preparation and evaluation of drug
containing poly(dl-lactide) microspheres
formed by the solvent evaporation
method. Pharmaceutical Research,
;4:465–471.
Ogawa Y, Yamamoto M, Okada H,
Yashiki T, Shimamoto T. Nanoparticle
preparation by high-pressure
emulsification: A new technique to
efficiently entrap leuprolide acetate into
microcapsules of polylactic acid or
copoly(lactic/glycolic) acid. Chemical and
Pharmaceutical Bulletin, 1988;36:1095–
Conti B, Genta I, Modena T, Pavanetto F.
Investigation on process parameters
involved in polylactic-co-glycolic
microspheres preparation. Drug
Development and Industrial Pharmacy,
;21:615–622.
Jalil R, Nixon JR. Biodegradable poly
(lactic acid) and poly (lactidecoglycolide) microcapsules: problems
associated withpreparative techniques and
release properties. Journal of
Microencapsulation, 1990;7:297–325.
Schwarz C, Mehnert W, Lucks JS, Muller
RH. Solid lipid nanoparticles (SLN) for
controlled drug delivery. I. Production,
characterization and sterilization. Journal
of Controlled Release, 1994;30:83–96.
Jumaa M, Muller BW. The effect of oil
components and homogenization
conditions on the physicochemical
properties and stability of parenteral fat
emulsions. International Journal of
Pharmaceutics, 1998;163:81–89.
Teixeira H, Dubernet C, Puisieux F,
Benita S, Couvreur P. Submicron cationic
emulsions as a new delivery system for
oligonucleotides. Pharmaceutical
Research, 1999;16:30–36.
Washington C, Davis SS. The production
of parenteral feeding emulsions by
Microfluidizer. International Journal of
Pharmaceutics, 1988;44:169–176.
Bachmann D, Brandl M, Gregoriadis G.
Preparation of liposomes using a MiniLab 8.30 H high-pressure homogenizer.
International Journal of Pharmaceutics,
;91:69–74.
Chen RH, Win HP, Fang HJ. Vesicle size,
size distribution, stability, and rheological
properties of liposomes coated with
water-soluble chitosans of different
molecular weights and concentrations.
Journal of liposome research,
;11:211–228.
Lamprecht A, Ubrich N, Hombreiro Perez
M, Lehr CM, HoFFman M, Maincent P.
Influences of process parameters on
nanoparticle preparation performed by a
double emulsion pressure homogenization
technique. International Journal of
Pharmaceutics, 2000;196:177–182.
Ueda M, Kreuter J. Optimization of the
preparation of loperamide-loaded poly(llactide) nanoparticles by high pressure
emulsification-solvent evaporation.
Journal of Microencapsulation,
;14:593–605.
Zimmer A, Kreuter J. Microspheres and
nanoparticles used in ocular delivery
systems. Advanced Drug Delivery
Reviews, 1995;16:61–73.
Calvo P, Alonso MJ, Vita-Jato JL,
Robinson JR. Improved ocular
bioavailability of indomethacin by novel
ocular drug carriers. Journal of Pharmacy
and Pharmacology, 1996;48:1147–1152.
Zimmer A, Chetoni P, Saettone M, Zerbe
H, Kreuter J. Evaluation of budesonideloaded albumin particles as controlled
drug delivery systems for the eye. II. Coadministration with bioadhesive and
viscous polymers. Journal of Controlled
Release, 1995;33:31–46.
Dinda I, Biswal S, Kumar Si S, Barik BB.
Budesonide Loaded PLGA-Nanoparticles:
Effect of Stabilizers and Process
Parameters. International Journal of Drug
Formulation & Research, 2011;2(1):206–
Soriano I, Delgado A, Diaz RV, Evora C.
Use of surfactants in polylactic acid
protein microspheres. Drug Development
and Industrial Pharmacy, 1995;21:549– 558.