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Preparation and characterization of poly(lactic acid) nanoparticles for sustained release of pyridostigmine bromide.


A novel pyridostigmine bromide poly (lactic acid) nanoparticles (PBPNPs) was prepared to obtain sustained release characteristics of PB. A central composite design approach was employed for process optimization. The in vitro release studies were carried out by dialysis method and conducted using four different dissolution media. Similar factor method was investigated for dissolution profile comparison. Multiple linear regression analysis for process optimization revealed that the optimal PBPNPs were obtained where the values of the amount of PB (X1, mg), PLA concentration (X2, % w:v), and PVA concentration (X3, % w:v) were 49.20 mg, 3.31% and 3.41%, respectively. The average particle size and zeta potential of PBPNPs with the optimized formulation were 722.9 +/- 4.3 nm, and -25.12 +/- 1.2 mV, respectively. PBPNPs provided an initial burst of drug release followed by a very slow release over an extended period of time (72 h). Compared with free PB, PBPNPs had a significantly lower release rate of PB in vitro. The in vitro release profile of the PBPNPs could be described by Weibull models, regardless of type of dissolution medium. Statistical significance of similarity between every two dissolution profiles of PBPNPs in different dissolution media was found, and the difference between the curves of PBPNPs and pure PB was statistically significant.


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  • Authors+Show Affiliations


    Department of Thoracic Surgery, Institute of Surgery, Third Military Medical University, Chongqing PR China.

    , , ,


    Die Pharmazie 67:4 2012 Apr pg 311-8


    Chemistry, Pharmaceutical
    Cholinesterase Inhibitors
    Delayed-Action Preparations
    Drug Carriers
    Indicators and Reagents
    Lactic Acid
    Models, Statistical
    Particle Size
    Pyridostigmine Bromide
    Reproducibility of Results
    Spectrophotometry, Ultraviolet
    Spectrum Analysis

    Pub Type(s)

    Journal Article
    Research Support, Non-U.S. Gov't



    PubMed ID