Journal of Drug Delivery Science and Technology, Volume (47), Year (2018-7) , Pages (95-105)

Title : ( An in-situ forming implant formulation of naltrexone with minimum initial burst release using mixture of PLGA copolymers and ethyl heptanoate as an additive: In-vitro, ex-vivo, and in-vivo release evaluation )

Authors: H. Kamali , E. Khodaverdi , F. Hadizadeh , R. Yazdian-Robati , A. Haghbin , Gholamhossein Zohuri ,

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Abstract

An in-situ forming implant formulation of naltrexone (NTX) was achieved based on a minimum initial burst release of NTX in the in-vitro release medium using a Box-Behnken design. Variables such as percent of copolymer by weight, copolymer composition (PLGA 756s: PLGA 504H), and percent ethyl heptanoate by weight as an additive in formulation were investigated. The in-vitro, ex-vivo, and in-vivo release of the optimized formulation was investigated. The rabbit-blood concentrations of the optimized formulation and Vivitrol were compared to ensure their equivalency. The initial burst release of the optimized formulation in the in-vitro release over the first 24 h, 6.18 ± 0.91%, was significantly (p < 0.05) lower than that of the formulation containing 100% of PLGA 504H (17.45 ± 1.07%) and 100% of PLGA 756s (11.82 ± 1.03%). The C max ® of NTX (21.06 ± 2.9 ng/mL) from the optimized formulation was close to that of Vivitrol® (21.11 ± 2.89 ng/mL). Also, the absolute bioavailability (F) and the range of serum concentration of NTX (C) of the ISFI formulation (F =18.29, C =6.18–22.84) were similar to Vivitrol ® (F =16.83, C =6.83–23.09). These results indicate that the optimized formulation can reach an effective therapeutic concentration for treating opioid and alcohol dependence.

Keywords

, Keywords: PLGA, Initial burst release, In situ forming implant, Optimized formulation, Naltrexone
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@article{paperid:1069266,
author = {H. Kamali and E. Khodaverdi and F. Hadizadeh and R. Yazdian-Robati and A. Haghbin and Zohuri, Gholamhossein},
title = {An in-situ forming implant formulation of naltrexone with minimum initial burst release using mixture of PLGA copolymers and ethyl heptanoate as an additive: In-vitro, ex-vivo, and in-vivo release evaluation},
journal = {Journal of Drug Delivery Science and Technology},
year = {2018},
volume = {47},
month = {July},
issn = {1773-2247},
pages = {95--105},
numpages = {10},
keywords = {Keywords: PLGA; Initial burst release; In situ forming implant; Optimized formulation; Naltrexone},
}

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%0 Journal Article
%T An in-situ forming implant formulation of naltrexone with minimum initial burst release using mixture of PLGA copolymers and ethyl heptanoate as an additive: In-vitro, ex-vivo, and in-vivo release evaluation
%A H. Kamali
%A E. Khodaverdi
%A F. Hadizadeh
%A R. Yazdian-Robati
%A A. Haghbin
%A Zohuri, Gholamhossein
%J Journal of Drug Delivery Science and Technology
%@ 1773-2247
%D 2018

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