One of the most popular techniques for the preparation of PLGA nanoparticles is emulsification solvent evaporation and its modifications such as the use of a double emulsion for the encapsulation of water soluble drugs. 1,2) In the current study, a homogenisation step was added to the preparation procedure. The effect of the stirring speed used during emulsification on the PLGA particle properties has been extensively examined.3,4) However, high stirring speed and even sonication are often not sufficient to achieve a small particle size and/or a narrow particle size distribution. Therefore, the high-pressure homogenisation technique was successfully adapted.5) This method is mainly used for the production of microemulsions [6][7][8] and liposomes, 9,10) but there is only a limited number of studies concerning polymeric nanoparticle preparations.
11-13)The particle size is, however, an important parameter codetermining the particle distribution and drug release. More specifically for ophthalmic use, it has been observed that large particles may irritate the eye. Consequently, smaller particles are preferred for ophthalmic delivery systems.
14)Additionally, Calvo et al. have reported that poly(e-caprolactone) nanoparticles (0.20-0.25 mm) improve ocular bioavailibility of indomethacin rather than poly(e-caprolactone) microparticles (6 mm).15) Thus, one of the most important characteristics of nanoparticles is their size.The present study aimed to evaluate the feasibility of homogenisation as a tool to adapt the properties of pilocarpine HCl-loaded PLGA nanoparticles. The influence of the homogenisation procedure on the size, the zeta potential value, drug encapsulation and drug release of the particles prepared was studied.The homogenisation parameters studied were the pressure applied, as well as the number of cycles.PLGA particles were prepared using three different stabilisers: polyvinylalcohol (PVA), carbomer (Carbopol 980 NF) and poloxamer (Lutrol F-68). PVA is the reference stabilising agent for the emulsification-solvent evaporation method.3) The feasibility of the use of Carbopol and poloxamer has been demonstrated in earlier work.16) Apart from these three stabilisers, mixtures of PVA and poloxamer as well as mixtures of PVA and Carbopol were also employed.The ocular bioavailibility can be improved using mucoadhesive particulate drug delivery systems.17) Various methods have been developed to evaluate the mucoadhesion of nanoparticulate drug delivery systems. Determination of the detachment force for microspheres from pig intestinal mucosa 18) or from mucus model gel 19) was proposed. Another method was to evaluate the amount of attached or non-adherent nanoparticles after placing on the rat intestinal mucosa.
20)Some authors investigated the behaviour of mucin/bioadhesive polymer dispersions by rheology 21,22) or by turbidimetric measurements.23) Thus, the interaction between mucin and mucoadhesive products caused changes in the viscosity or turbidity of the dispersions. Since these techniques are easily ...