An in vivo/in vitro comparison with a leuprolide osmotic implant for the treatment of prostate cancer

Wright, Jeremy C.; Leonard, Sally Tao; Stevenson, Cynthia L.; Beck, James C.; Chen, Guohua; Jao, Rose Marie; Johnson, Paul A.; Leonard, Joe C.; Skowroński, Roman

doi:10.1016/s0168-3659(01)00358-3

Cited by 74 publications

(59 citation statements)

References 15 publications

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“…16 Preferred rate modifying agents are dimethyl citrate, triethyl citrate, ethyl heptanoate, [17][18][19] glycerin, and hexanediol. 20 These substances are biocompatible and approved by FDA.…”

Section: Introductionmentioning

confidence: 99%

Effect of additives on release profile of leuprolide acetate in an in situ forming controlled‐release system: In vitro study

Zare

Mobedi

Barzin

et al. 2007

J of Applied Polymer Sci

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In situ forming drug delivery system is prepared by phase inversion technique using poly (D,L-lacticco-glycolide) and leuprolide acetate dissolved in N-methyl-2-pyrrolidone. The effects of ethyl heptanoate and glycerol additives are important determinant as rate modifying agents on the drug release kinetics in biodegradable in situ forming porous systems of poly(D,L-lactide-co-glycolide) (PLGA) in N-methyl-2-pyrrolidone (NMP). The release performance and porous structure morphology are investigated by scanning electron microscopy and UV-visible spectroscopy techniques to study the effect of additives. The experimental results exhibit the crucial role of ethyl heptanoate and glycerol at different loadings (1, 3, and 5% w/w) on release profile of leuprolide acetate loaded on poly(D,L-lactide-co-glycolide)hydroxylated (PLGA-H). Both additives at different concentrations reduce the burst effect, while increasing duration of drug release. Ethyl heptanoate, however, shows stronger effect than glycerol. The results of morphological studies show that ethyl heptanoate reduces the porosity of the polymer surface and interconnected tear-like structures of the bulk disappear while the sponge-like structures are observed. In this system glycerol reduces the surface porosity intensively, while the interconnected tears change into channel-like structures. Therefore, morphological results confirm the effect of additives on leuprolide release profile.

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Section: Introductionmentioning

confidence: 99%

Effect of additives on release profile of leuprolide acetate in an in situ forming controlled‐release system: In vitro study

Zare

Mobedi

Barzin

et al. 2007

J of Applied Polymer Sci

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“…Remarkably, the fluctuation of plasma concentration for this osmotic pump subcutaneous infusion system was significantly smaller, compared with intravenous injection, which were similar to osmotic micropump or subcutaneous infusion (Mikkelsen Lynch et al, 2000;Fisher et al, 2003;Herrmanna et al, 2009). Steady drug serum levels produced by this delivery device would result in the desired pharmacodynamic efficacy and mild adverse effects (Mikkelsen Lynch et al, 2000;Wright et al, 2001). The AUC (0-12) for subcutaneous infusion was essentially equal to that for intravenous injection (46.11 AE 0.59 mgÁh/mL for intravenous injection and 42.98 AE 2.09 mgÁh/mL for subcutaneous infusion).…”

Section: In Vivo Studymentioning

confidence: 85%

A novel subcutaneous infusion delivery system based on osmotic pump:in vitroandin vivoevaluation

Gong¹,

Danyu³

et al. 2013

Drug Delivery

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School of Pharmacy, Zhejiang University, Hangzhou, P.R. China AbstractAn economical, convenient portable drug delivery system combining osmotic pump with subcutaneous infusion was developed, which was composed of three primary components: water chamber, osmotic pump chamber and support base. Ceftriaxone sodium (CRO) was selected as the model drug and osmotic pump tablets were prepared. The influence of osmotic agents on drug release profiles was evaluated. As the adjustment made by the osmotic agents was limited, the compositions of semipermeable membrane were investigated to determine significant associations of factors based on orthogonal design. The in vitro release profiles of the optimum formulation achieved to the predetermined value (15 AE 3 min for the initial release time T i and 5.75 AE 0.25 h for the extent release time T e ). The pharmacokinetic profiles of this drug delivery system were evaluated in Beagle dogs. In vivo results demonstrated that the osmotic pump subcutaneous infusion administration was equivalent to intravenous injection administration in terms of bioavailability. Moreover, constant drug plasma levels with minimized fluctuations could be achieved with this osmotic pump subcutaneous infusion system, compared with intravenous injection.

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“…The fluctuation of plasma concentration for the developed pump was similar to the reference commercial pump. Steady drug plasma levels produced by this delivery device would result in the desired pharmacodynamic efficacy and mild adverse effects (Wright et al, 2001). The AUC (0-t) of developed pump and reference one was 111.60 ± 18.65 and 104.72 ± 16.49 mgÁh/mL, respectively.…”

Section: In Vivo Studymentioning

confidence: 97%

The development and evaluation of a subcutaneous infusion delivery system based on osmotic pump control and gas drive

Xie

Yang²,

Yang³

et al. 2014

Drug Delivery

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(2016) The development and evaluation of a subcutaneous infusion delivery system based on osmotic pump control and gas drive, Drug Delivery, 23:7, 2193-2204, DOI: 10.3109/10717544.2014 AbstractA novel, self-administration drug delivery system for subcutaneous infusion was developed and evaluated. The device includes two main components: an osmotic tablet controlled gas actuator and a syringe catheter system. The sodium carbonate in the osmotic pump tablet will release into the surround citric acid solution and produce CO 2 gas, which will drive the drug solution into subcutaneous tissue. The key formulation factors of the osmotic tablet that would influence the infusion profiles of the device were investigated by single factor exploration. The formulation was optimized via a response surface methodology. With an 18 ± 4 min of lag time, the delivery system was able to infuse at an approximate zero-order up to 5.90 ± 0.37 h with a precision of 9.0% RSD (n ¼ 6). A linear correlation was found for the infusion profile and the fitting equation was Y ¼ 0.014X À 0.004 (r ¼ 0.998). A temperature change of 4 C was found to modify the flow rate by about 12.0%. In vivo results demonstrated that the present subcutaneous infusion device was similar to the commercial infusion pump, and it could bring a long and constant ampicillin plasma level with minimized fluctuations.

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An in vivo/in vitro comparison with a leuprolide osmotic implant for the treatment of prostate cancer

Cited by 74 publications

References 15 publications

Effect of additives on release profile of leuprolide acetate in an in situ forming controlled‐release system: In vitro study

Effect of additives on release profile of leuprolide acetate in an in situ forming controlled‐release system: In vitro study

A novel subcutaneous infusion delivery system based on osmotic pump:in vitroandin vivoevaluation

The development and evaluation of a subcutaneous infusion delivery system based on osmotic pump control and gas drive

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