Poly (D, L-Lactide) Nanosuspensions of Risperidone for Parenteral Delivery: Formulation and In-Vitro Evaluation

Abstract

Risperidone, an "atypical" antipsychotic drug, having large scope for prolonged psychotic treatments through novel parenteral drug delivery systems. Polymeric nanoparticles suspensions containing risperidone made of poly (D, L-Lactide) were designed by nanoprecipitation method using polymeric stabilizer (Pluronic F-68 or Pluronic F-127). The prepared nanosuspensions were characterized for particle size by photon correlation spectroscopy and scanning electron microscopy. The free dissolved drug in the nanosuspension was determined by bulk equilibrium reverse dialysis bag technique. In vitro release studies were carried out using dialysis bag diffusion technique. The particle size of the prepared nanoparticles in the nanosuspensions ranged between 78-184 nm. Nanoparticles of risperidone in the nanosuspensions were obtained with high encapsulation efficiency (91-94 %). The drug release from the risperidone nanosuspension was sustained in some batches for more than 24 h with 75% drug release whereas release from risperidone solution showed release within 1.5 h. The release pattern of drug is analyzed and found to follow first order equation and Fickian diffusion kinetics. These studies suggest the feasibility of formulating risperidone loaded poly (D, L-Lactide) nanoparticles suspension for the treatment of psychotic disorders.

A Review of In Vitro Drug Release Test Methods for Nano-Sized Dosage Forms

“…the nanoparticles are introduced into a dialysis bag containing release media (inner media/compartment) that is subsequently sealed and placed in a larger vessel containing release media (outer media/compartment), agitated to minimize unstirred water layer effects [32,55]. In general, the volume enclosed in a dialysis bag (inner media) is significantly smaller than the outer media.…”

“…In general, the volume enclosed in a dialysis bag (inner media) is significantly smaller than the outer media. For instance, inner media volumes reported in literature range from 1 to 10 mL, whereas the outer media volume is much greater, typically around 40-90 mL [32,53,55]. Thus, container size will depend on the total volume of release media required for the in vitro release study.…”

“…However, the rationale for selecting a MWCO is rather subjective. For instance, a MWCO as high as 10-14 kDa was used to study drug release of small molecules like Risperidone and Indomethacin, and a MWCO as low as 1 kDa though suitable for assessing in vitro release of a large molecule, pDNA, proved to be limiting for the diffusion of Cefuroxime Axetil, a cephalosporin antibiotic [32,38,55,60]. In general, the MWCO should be sufficiently large to permit drug transport.…”

SLNs Based on Co-Processed Lipids for Topical Delivery of Terbinafine Hydrochloride

“…High zeta-potential values should be achieved to ensure a high energy barrier and to favor good stability. Nanoparticles with zeta potential values between +30 to -30 mV typically have high degrees of stability [30,31]. Our zeta-potential results suggested that poloxamer 188 concentration was sufficient to cover the surface of the nanoparticles effectively (Table 3).…”

Synergistic and complete reversal of the multidrug resistance of mitoxantrone hydrochloride by three-in-one multifunctional lipid-sodium glycocholate nanocarriers based on simultaneous BCRP and Bcl-2 inhibition

“…It was investigated that 85.7% of MTO was released from the MTO-TMLGNs after 72 hours, while almost 100% was released from MTO-Sol after 4 hours. It was possible that ionic interaction and complexation between the MTO and carrageenan was so strong Numerous methods for release determination are reported in the literature including dialysis-based methods, [35][36][37] ultracentrifugation, 38,39 centrifugal ultrafiltration, 40 and pressure ultrafiltration. 41,42 However, to our knowledge, no method is perfect for the release study to date.…”