Screening of mucoadhesive microparticles containing hydroxypropyl-beta-cyclodextrin for the nasal delivery of risperidone.
نویسندگان
چکیده
Interaction of the antipsychotic drug risperidone with hydroxypropyl-beta-cyclodextrin (HPBCD) in solution and in the solid state was studied with the aim of overcoming the limitations associated with nasal administration of low solubility drugs. Risperidone solubility studies revealed inclusion complex formation with a 1:1 stoichiometry. Low concentrations (0.1 w/v %) of hydroxypropylmethyl cellulose (HPMC) and carbomer affected risperidone solubility in water. No formation of a ternary complex was detected. The solid inclusion complex was prepared by spray drying and was characterised by thermal (DSC) and spectral (FTIR) analyses. Risperidone and the inclusion complex were loaded into microparticles by spray drying using HPMC, carbomer and HPMC/carbomer interpolymer complex (IPC) as mucoadhesive components. The microparticles were characterised with respect to drug loading, particle size distribution, thermal analysis, and zeta potential measurements. Mucoadhesive properties of the microparticles were studied by measuring the work of adhesion. Carbomer and IPC based microparticles revealed superior mucoadhesive microparticles compared to HPMC based microparticles. Drug incorporation into microparticles reduced their mucoadhesive properties, while incorporation of the cyclodextrin complex caused no additional reduction in mucoadhesion. The in vitro dissolution studies showed that formation of the inclusion complex significantly increased the risperidone dissolution rate from the microparticles, thus providing sustained drug release.
منابع مشابه
Formulation and Evaluation of In-vitro Characterization of Gastic-Mucoadhesive Microparticles/Discs Containing Metformin Hydrochloride
The present study involves preparation and evaluation of gastric-mucoadhesive microparticles with Metformin Hydrochloride as model drug for prolongation of gastric residence time. The microparticles were prepared by the emulsification solvent evaporation technique using polymers of Carbomer 934p (C) and Ethylcellulose (EC). The microparticles were prepared by emulsion solvent evaporation method...
متن کاملFormulation and Evaluation of In-vitro Characterization of Gastic-Mucoadhesive Microparticles/Discs Containing Metformin Hydrochloride
The present study involves preparation and evaluation of gastric-mucoadhesive microparticles with Metformin Hydrochloride as model drug for prolongation of gastric residence time. The microparticles were prepared by the emulsification solvent evaporation technique using polymers of Carbomer 934p (C) and Ethylcellulose (EC). The microparticles were prepared by emulsion solvent evaporation method...
متن کاملDevelopment and Characterization of Paracetamol Complexes with Hydroxypropyl-?-Cyclodextrin
Paracetamol is a sparingly soluble bitter tasting drug. It is widely used as an analgesic and antipyretic. Complexation of drug with different cyclodextrins (?, ? and HP-?-CD) was attempted to improve solubility of Paracetamol. During the drug excipient interaction studies, ?, ? cyclodextrins elicited analytical interference and showed considerable absorbance at ?max (243.5 nm) of Paracetamol w...
متن کاملPreparation and in-vitro evaluation of sodium alginate microspheres containing diphtheria toxoid as new vaccine delivery
During last two decades, polysaccharides such as alginate (Alg) alone and in combination with other biopolymers are widely used in vaccine and drug delivery systems. The aim of the present work was to investigate the potential utility of microparticles made of alginate (Alg) as new vehicles for improving nasal vaccine delivery. For this purpose, diphtheria toxoid (DT) was chosen as a model an...
متن کاملDevelopment and Characterization of Paracetamol Complexes with Hydroxypropyl-?-Cyclodextrin
Paracetamol is a sparingly soluble bitter tasting drug. It is widely used as an analgesic and antipyretic. Complexation of drug with different cyclodextrins (?, ? and HP-?-CD) was attempted to improve solubility of Paracetamol. During the drug excipient interaction studies, ?, ? cyclodextrins elicited analytical interference and showed considerable absorbance at ?max (243.5 nm) of Paracetamol w...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید
ثبت ناماگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید
ورودعنوان ژورنال:
- Combinatorial chemistry & high throughput screening
دوره 10 5 شماره
صفحات -
تاریخ انتشار 2007