Pharmacokinetics and in vitro and in vivo correlation of huperzine A loaded poly(lactic-co-glycolic acid) microspheres in dogs

Chu, Dafeng; Fu, Xueqi; Liu, Wanhui; Liu, Ke; Li, Youxin

doi:10.1016/j.ijpharm.2006.06.032

Cited by 68 publications

(35 citation statements)

References 32 publications

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“…The in vitro and in vivo correlation (IVIVC) is an important issue for parenteral biodegradable depot systems as well as for oral dosage forms [18,19] . A proper IVIVC can be used to predict an in vivo release profile for parenteral biodegradable depot systems with the aid of an in vitro release profile conducted in PBS.…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetic and pharmacodynamic profiles of recombinant human erythropoietin-loaded poly(lactic-co-glycolic acid) microspheres in rats

Zhou

et al. 2011

Acta Pharmacol Sin

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Aim: To characterize the pharmacokinetic and pharmacodynamic profiles of the recombinant human erythropoietin (rhEPO)-loaded poly(lactic-co-glycolic acid) (PLGA) microspheres in rats. Methods: The rhEPO-loaded microspheres were prepared using a solid-in-oil-in-water emulsion method. Pharmacokinetics and pharmacodynamics of the rhEPO-loaded microspheres were evaluated in male Sprague-Dawley rats. The serum rhEPO level was determined with ELISA. The level of anti-rhEPO antibody in the serum was measured to assess the immunogenicity of rhEPO released from the microspheres. Results: rhEPO was almost completely released from the PLGA microspheres in vitro, following zero-order release kinetics over approximately 30 d. After intramuscular injection (10 000 or 30 000 IU rhEPO/kg) in the rats, the serum rhEPO concentration reached maximum levels on d 1, then decreased gradually and was maintained at nearly steady levels for approximately 4 weeks. Furthermore, the release of rhEPO from the PLGA microspheres was found to be controlled mainly by a dissolution/diffusion mechanism. A good linear correlation (R 2 =0.98) was obtained between the in vitro and in vivo release data. A single intramuscular injection of the rhEPOloaded PLGA microspheres (10 000 or 30 000 IU rhEPO/kg) in the rats resulted in elevated hemoglobin and red blood cell concentrations for more than 28 d. Moreover, the immunogenicity of rhEPO released from the PLGA microspheres was comparable with that of the unencapsulated rhEPO. Conclusion:The results prove the feasibility of using the PLGA-based microspheres to deliver rhEPO for approximately 1 month.

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Section: Discussionmentioning

confidence: 99%

Pharmacokinetic and pharmacodynamic profiles of recombinant human erythropoietin-loaded poly(lactic-co-glycolic acid) microspheres in rats

Zhou

et al. 2011

Acta Pharmacol Sin

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“…Recently, several studies reported the use of biodegradable microspheres to sustain the delivery of huperzine A, a natural AChE inhibitor isolated from the Chinese herb Huperzia serrata and approved for human use in China [44,45]. In rat [44,46] and dog models [47], it was found that the s.c. injection of huperzine A-loaded microspheres provided therapeutic plasma drug levels for ca. 15-60 days, and inhibited the rat cerebral cortex AChE by 10-20%.…”

Section: Discussionmentioning

confidence: 99%

Tyrosine-based rivastigmine-loaded organogels in the treatment of Alzheimer’s disease

et al. 2010

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Organogels can be prepared by immobilizing an organic phase into a three-dimensional network coming from the self-assembly of a low molecular weight gelator molecule. In this work, an injectable subcutaneous organogel system based on safflower oil and a modified-tyrosine organogelator was evaluated in vivo for the delivery of rivastigmine, an acetylcholinesterase (AChE) inhibitor used in the treatment of Alzheimer's disease. Different implant formulations were injected and the plasmatic drug concentration was assayed for up to 35 days. In parallel, the inhibition of AChE in different brain sections and the biocompatibility of the implants were monitored. The pharmacokinetic profiles were found to be influenced by the gel composition, injected dose and volume of the implant. The sustained delivery of rivastigmine was accompanied by a significant prolonged inhibition of AChE in the hippocampus, a brain structure involved in memory. The implant induced only a minimal to mild chronic inflammation and fibrosis, which was comparable to poly(D,L-lactide-co-glycolide) in situ-forming implants. These findings suggest that tyrosine-based organogels could represent an alternative approach to current formulations for the sustained delivery of cholinesterase inhibitors.

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“…The fraction of drug absorbed/released then increased gradually after day 15 and a plateau was reached by day 27, which was faster than the real-time in vitro release profile (plateaued by day 36). Faster in vivo risperidone release may be a result of enhanced PLGA microsphere degradation due to change in the release mechanism from bulk erosion to surface erosion, as a consequence of lower local pH conditions [20,23] and/or the presence of biological components (e.g. enzymes [36]).…”

Section: In Vivo Studies Of the Risperidone Microspheresmentioning

confidence: 99%

“…bi-or tri-phasic release profiles), deconvolution of in vivo data and correlation with in vitro release data have been challenging. Until now, there are only a few literature reports on the establishment of IVIVCs for parenteral polymeric microspheres, albeit with different in vitro release testing approaches, such as the USP 4 method [19,20], dialysis based methods [17,18], as well as sample-and-separate methods [21][22][23]. None of these has addressed the importance of developing an IVIVC for compositionally equivalent PLGA microspheres with manufacturing differences.…”

Section: Introductionmentioning

confidence: 99%

In vitro-in vivo correlation of parenteral risperidone polymeric microspheres

Shen

Choi

et al. 2015

Journal of Controlled Release

101

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The objective of the present study was to determine whether an in vitro-in vivo correlation (IVIVC) can be established for polymeric microspheres that are equivalent in formulation composition but prepared with different manufacturing processes. Risperidone was chosen as a model therapeutic and poly(lactic-co-glycolic acid) (PLGA) with similar molecular weight as that used in the commercial product Risperdal ® Consta ® was used to prepare risperidone microspheres. Various manufacturing processes were investigated to produce the risperidone microspheres with similar drug loading (approx. 37%) but distinctly different physicochemical properties (e.g. porosity, particle size and particle size distribution). In vitro release of the risperidone microspheres was investigated using different release testing methods (such as sampleand-separate and USP apparatus 4). In vivo pharmacokinetic profiles of the risperidone microsphere formulations following intramuscular administration were determined using a rabbit model. Furthermore, the obtained pharmacokinetic profiles were deconvoluted using the LooRiegelman method and the calculated in vivo release was compared with the in vitro release of these microspheres. Level A IVIVCs were established and validated for the compositionally equivalent risperidone microspheres based on the in vitro release data obtained using USP apparatus 4. The developed IVIVCs demonstrated good predictability and were robust. These results showed that the developed USP apparatus 4 method was capable of discriminating PLGA microspheres that are equivalent in formulation composition but with manufacturing differences and predicting their in vivo performance in the investigated animal model.

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Pharmacokinetics and in vitro and in vivo correlation of huperzine A loaded poly(lactic-co-glycolic acid) microspheres in dogs

Cited by 68 publications

References 32 publications

Pharmacokinetic and pharmacodynamic profiles of recombinant human erythropoietin-loaded poly(lactic-co-glycolic acid) microspheres in rats

Pharmacokinetic and pharmacodynamic profiles of recombinant human erythropoietin-loaded poly(lactic-co-glycolic acid) microspheres in rats

Tyrosine-based rivastigmine-loaded organogels in the treatment of Alzheimer’s disease

In vitro-in vivo correlation of parenteral risperidone polymeric microspheres

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