The inclusion complex formation of lorazepam and risperidone with HP-β-CD in solution and in solid state was investigated. In solutions of different pH values risperidone and lorazepam formed inclusion complexes with HP-β-CD. The inclusion complex formation significantly increased risperidone and lorazepam solubility. Media pH value and presence of the polymers (hydroxypropylmethyl cellulose (HPMC) and carbomer) influenced the stability of inclusion complexes. Inclusion complexes of risperidone and lorazepam in solid state were prepared by spray drying and characterised by differential scanning calorimetry (DSC) and FTIR spectroscopy. Lorazepam, risperidone and their inclusion complexes were incorporated in the mucoadhesive microparticles by spray drying. HPMC, carbomer and interpolymer complex of HPMC and carbomer were used as mucoadhesive components. Prepared microparticles were characterised by determination of drug content, particle size distribution, zeta potential measurement and DSC measurement. Mucoadhesion of the microparticles was investigated by in situ method based on adhesion work measurement. Chemical structure of the polymers and drug entrapment affected the mucoadhesion of the microparticles, while HP-β-CD effect was negligible. In vitro drug release form microparticles was limited by low water solubility of lorazepam and risperidone. The drug release mechanism included the drug diffusion through hydrated polymer matrix and matrix erosion. HP-β-CD affected the lorazepam release rate by increasing the drug solubility in swollen polymer matrix of the microparticles. HP-β-CD also promoted the matrix erosion and therefore contributed to the drug release. The same mechanism controlled the risperidone release from HPMC microparticles containing HP-β-CD. The drug-carbomer interaction limited the release of risperidone from the microparticles formulated with carbomer and interpolymer complex. Therefore, the influence of HP-β-CD on drug release from this microparticles was less pronounced. The in vitro diffusion studies were performed using standard Franz-diffusion cell. Thereby nasal absorption of the drugs was simulated. Inclusion complex formation affected lorazepam and risperidone diffusibility by increasing the drug solubility. HP-β-CD acted as a carrier of the lipophilic drugs across the hydrodynamic layer on the membrane surface and increased the drug concentration gradient over the membrane. HP-β-CD in microparticles changed the values of in vitro drug diffusion. Inclusion complex formation affected the drug release rate from the microparticles and therefore higher concentrations of lorazepam and risperidone were available for the diffusion. Above-mentioned characteristics of the mucoadhesive microparticles offer the potential for nasal application of lorazepam and risperidone and their transport to the cerebrospinal fluid and the brain. Cyclodextrins and investigated polymers in lorazepam and risperidone microparticles could formulate suitable drug delivery system for nasal application of psychoactive drugs.