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Marković, Bojan D. - One of the best experts on this subject based on the ideXlab platform.

  • Estimation of passive gastrointestinal absorption and membrane retention using PAMPA test, quantitative structure-permeability and quantitative structure-retention relationship analyses of ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid and 1,
    Elsevier B.V., 2020
    Co-Authors: Tubić, Biljana K., Dobričić Vladimir, Poljarević Jelena, Savić Aleksandar, Sabo Tibor, Marković, Bojan D.
    Abstract:

    Passive gastrointestinal absorption and membrane retention of twelve esters of (S,S)-ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid (EDCP) and (S,S)-1,3-propanediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid (PDCP), as well as of these two non-esterified acids were estimated using PAMPA test. Artificial PAMPA membrane used in this study for the simulation of gastrointestinal barrier was solution of Egg Lecithin in dodecane (1 % w/v). All tested compounds belong to class III (high membrane retention and low permeation), whereas EDCP, dipentyl ester of PDCP (DPE-PDCP) and diisopentyl ester of PDCP (DIPE-PDCP) belong to class I (negligible membrane retention and low permeation). Finally, quantitative structure – permeability and structure – retention relationships models were created in order to find quantitative relationships between physico-chemical properties of tested compounds and PAMPA membrane permeability/membrane retention parameters. Statistically the most reliable models were analysed and used for the design of new compounds for which favourable membrane permeability and retention can be expected.Supplementary material: [http://cherry.chem.bg.ac.rs/handle/123456789/3870]This is the peer-reviewed version of the following article: Tubić, B.; Dobričić, V.; Poljarević, J.; Savić, A.; Sabo, T.; Marković, B. Estimation of Passive Gastrointestinal Absorption and Membrane Retention Using PAMPA Test, Quantitative Structure-Permeability and Quantitative Structure-Retention Relationship Analyses of Ethylenediamine-N,N’-Di-2-(3-Cyclohexyl)Propanoic Acid and 1,3-Propanediamine-N,N’-Di-2-(3-Cyclohexyl)Propanoic Acid Derivatives. Journal of Pharmaceutical and Biomedical Analysis 2020, 184. [https://doi.org/10.1016/j.jpba.2020.113213

  • Estimation of passive gastrointestinal absorption and membrane retention using PAMPA test, quantitative structure-permeability and quantitative structure-retention relationship analyses of ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid and 1,
    Elsevier B.V., 2020
    Co-Authors: Tubić, Biljana K., Dobričić Vladimir, Poljarević Jelena, Savić Aleksandar, Sabo Tibor, Marković, Bojan D.
    Abstract:

    Passive gastrointestinal absorption and membrane retention of twelve esters of (S,S)-ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid (EDCP) and (S,S)-1,3-propanediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid (PDCP), as well as of these two non-esterified acids were estimated using PAMPA test. Artificial PAMPA membrane used in this study for the simulation of gastrointestinal barrier was solution of Egg Lecithin in dodecane (1 % w/v). All tested compounds belong to class III (high membrane retention and low permeation), whereas EDCP, dipentyl ester of PDCP (DPE-PDCP) and diisopentyl ester of PDCP (DIPE-PDCP) belong to class I (negligible membrane retention and low permeation). Finally, quantitative structure – permeability and structure – retention relationships models were created in order to find quantitative relationships between physico-chemical properties of tested compounds and PAMPA membrane permeability/membrane retention parameters. Statistically the most reliable models were analysed and used for the design of new compounds for which favourable membrane permeability and retention can be expected.Peer-reviewed manuscript: [http://cherry.chem.bg.ac.rs/handle/123456789/3869]Supplementary material: [http://cherry.chem.bg.ac.rs/handle/123456789/3870

  • Biocompatible Nanoemulsions for Improved Aceclofenac Skin Delivery: Formulation Approach Using Combined Mixture-Process Experimental Design
    'Wiley', 2016
    Co-Authors: Isailovic Tanja, Marković, Bojan D., Dordevic Sanela, Ranđelović Danijela, Cekic Nebojsa, Lukić Milica, Pantelić Ivana, Daniels Rolf, Savić, Snežana D.
    Abstract:

    We aimed to develop Lecithin-based nanoemulsions intended for effective aceclofenac (ACF) skin delivery utilizing sucrose esters [sucrose palmitate (SP) and sucrose stearate (SS)] as additional stabilizers and penetration enhancers. To find the suitable surfactant mixtures and levels of process variables (homogenization pressure and number of cycles-high pressure homogenization manufacturing method) that result in drug-loaded nanoemulsions with minimal droplet size and narrow size distribution, a combined mixture-process experimental design was employed. Based on optimization data, selected nanoemulsions were evaluated regarding morphology, surface charge, drug-excipient interactions, physical stability, and in vivo skin performances (skin penetration and irritation potential). The predicted physicochemical properties and storage stability were proved satisfying for ACF-loaded nanoemulsions containing 2% of SP in the blend with 0%-1% of SS and 1%-2% of Egg Lecithin (produced at 50 degrees C/20 cycles/800 bar). Additionally, the in vivo tape stripping demonstrated superior ACF skin absorption from these nanoemulsions, particularly from those containing 2% of SP, 0.5% of SS, and 1.5% of Egg Lecithin, when comparing with the sample costabilized by conventional surfactant-polysorbate 80. In summary, the combined mixture-process experimental design was shown as a feasible tool for formulation development of multisurfactant-based nanosized delivery systems with potentially improved overall product performances

Marković Bojan - One of the best experts on this subject based on the ideXlab platform.

  • Estimation of passive gastrointestinal absorption and membrane retention using PAMPA test, quantitative structure-permeability and quantitative structure-retention relationship analyses of ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid and 1,
    'Elsevier BV', 2020
    Co-Authors: Tubić Biljana, Dobričić Vladimir, Poljarević Jelena, Savić Aleksandar, Sabo Tibor, Marković Bojan
    Abstract:

    Passive gastrointestinal absorption and membrane retention of twelve esters of (S,S)-ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid (EDCP) and (S,S)-1,3-propanediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid (PDCP), as well as of these two non-esterified acids were estimated using PAMPA test. Artificial PAMPA membrane used in this study for the simulation of gastrointestinal barrier was solution of Egg Lecithin in dodecane (1 % w/v). All tested compounds belong to class III (high membrane retention and low permeation), whereas EDCP, dipentyl ester of PDCP (DPE-PDCP) and diisopentyl ester of PDCP (DIPE-PDCP) belong to class I (negligible membrane retention and low permeation). Finally, quantitative structure – permeability and structure – retention relationships models were created in order to find quantitative relationships between physico-chemical properties of tested compounds and PAMPA membrane permeability/membrane retention parameters. Statistically the most reliable models were analysed and used for the design of new compounds for which favourable membrane permeability and retention can be expected.This is the peer-reviewed version of the following article: Tubić, B.; Dobričić, V.; Poljarević, J.; Savić, A.; Sabo, T.; Marković, B. Estimation of Passive Gastrointestinal Absorption and Membrane Retention Using PAMPA Test, Quantitative Structure-Permeability and Quantitative Structure-Retention Relationship Analyses of Ethylenediamine-N,N’-Di-2-(3-Cyclohexyl)Propanoic Acid and 1,3-Propanediamine-N,N’-Di-2-(3-Cyclohexyl)Propanoic Acid Derivatives. Journal of Pharmaceutical and Biomedical Analysis 2020, 184. [https://doi.org/10.1016/j.jpba.2020.113213

  • Estimation of passive gastrointestinal absorption and membrane retention using PAMPA test, quantitative structure-permeability and quantitative structure-retention relationship analyses of ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid and 1,
    'Elsevier BV', 2020
    Co-Authors: Tubić Biljana, Dobričić Vladimir, Poljarević Jelena, Savić Aleksandar, Sabo Tibor, Marković Bojan
    Abstract:

    Passive gastrointestinal absorption and membrane retention of twelve esters of (S,S)-ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid (EDCP) and (S,S)-1,3-propanediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid (PDCP), as well as of these two non-esterified acids were estimated using PAMPA test. Artificial PAMPA membrane used in this study for the simulation of gastrointestinal barrier was solution of Egg Lecithin in dodecane (1 % w/v). All tested compounds belong to class III (high membrane retention and low permeation), whereas EDCP, dipentyl ester of PDCP (DPE-PDCP) and diisopentyl ester of PDCP (DIPE-PDCP) belong to class I (negligible membrane retention and low permeation). Finally, quantitative structure – permeability and structure – retention relationships models were created in order to find quantitative relationships between physico-chemical properties of tested compounds and PAMPA membrane permeability/membrane retention parameters. Statistically the most reliable models were analysed and used for the design of new compounds for which favourable membrane permeability and retention can be expected.Peer-reviewed manuscript: [http://farfar.pharmacy.bg.ac.rs/handle/123456789/3553

George S Kobayashi - One of the best experts on this subject based on the ideXlab platform.

  • treatment of murine candidiasis and cryptococcosis with amphotericin b incorporated into Egg Lecithin bile salt mixed micelles
    Antimicrobial Agents and Chemotherapy, 1994
    Co-Authors: Janina Brajtburg, S Elberg, S J Travis, George S Kobayashi
    Abstract:

    Amphotericin B (AmB) with deoxycholate (Fungizone) and AmB incorporated into mixed micelles (AmB-mixMs) composed of Egg Lecithin with glycocholate, deoxycholate, or taurocholate were compared as treatments for murine infections. For mice infected with Candida albicans, treatment consisted of a single intravenous injection; for mice infected with Cryptococcus neoformans, treatment consisted of two intravenous injections. The maximal tolerated doses of AmB as Fungizone were 1.25 mg/kg of body weight in mice with candidiasis and 2.5 mg/kg of body weight in mice with cryptococcosis. The AmB-mixMs were nontoxic to mice at doses of 80 and 100 mg/kg of body weight and were therapeutically more active than the maximal tolerated dose of Fungizone in both models of infection. However, when Fungizone or AmB-mixMs were administered at equivalent doses of AmB, AmB-mixMs were more active in treating murine candidiasis, whereas Fungizone was more active in treating murine cryptococcosis.

Poljarević Jelena - One of the best experts on this subject based on the ideXlab platform.

  • Estimation of passive gastrointestinal absorption and membrane retention using PAMPA test, quantitative structure-permeability and quantitative structure-retention relationship analyses of ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid and 1,
    'Elsevier BV', 2020
    Co-Authors: Tubić Biljana, Dobričić Vladimir, Poljarević Jelena, Savić Aleksandar, Sabo Tibor, Marković Bojan
    Abstract:

    Passive gastrointestinal absorption and membrane retention of twelve esters of (S,S)-ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid (EDCP) and (S,S)-1,3-propanediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid (PDCP), as well as of these two non-esterified acids were estimated using PAMPA test. Artificial PAMPA membrane used in this study for the simulation of gastrointestinal barrier was solution of Egg Lecithin in dodecane (1 % w/v). All tested compounds belong to class III (high membrane retention and low permeation), whereas EDCP, dipentyl ester of PDCP (DPE-PDCP) and diisopentyl ester of PDCP (DIPE-PDCP) belong to class I (negligible membrane retention and low permeation). Finally, quantitative structure – permeability and structure – retention relationships models were created in order to find quantitative relationships between physico-chemical properties of tested compounds and PAMPA membrane permeability/membrane retention parameters. Statistically the most reliable models were analysed and used for the design of new compounds for which favourable membrane permeability and retention can be expected.This is the peer-reviewed version of the following article: Tubić, B.; Dobričić, V.; Poljarević, J.; Savić, A.; Sabo, T.; Marković, B. Estimation of Passive Gastrointestinal Absorption and Membrane Retention Using PAMPA Test, Quantitative Structure-Permeability and Quantitative Structure-Retention Relationship Analyses of Ethylenediamine-N,N’-Di-2-(3-Cyclohexyl)Propanoic Acid and 1,3-Propanediamine-N,N’-Di-2-(3-Cyclohexyl)Propanoic Acid Derivatives. Journal of Pharmaceutical and Biomedical Analysis 2020, 184. [https://doi.org/10.1016/j.jpba.2020.113213

  • Estimation of passive gastrointestinal absorption and membrane retention using PAMPA test, quantitative structure-permeability and quantitative structure-retention relationship analyses of ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid and 1,
    Elsevier B.V., 2020
    Co-Authors: Tubić, Biljana K., Dobričić Vladimir, Poljarević Jelena, Savić Aleksandar, Sabo Tibor, Marković, Bojan D.
    Abstract:

    Passive gastrointestinal absorption and membrane retention of twelve esters of (S,S)-ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid (EDCP) and (S,S)-1,3-propanediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid (PDCP), as well as of these two non-esterified acids were estimated using PAMPA test. Artificial PAMPA membrane used in this study for the simulation of gastrointestinal barrier was solution of Egg Lecithin in dodecane (1 % w/v). All tested compounds belong to class III (high membrane retention and low permeation), whereas EDCP, dipentyl ester of PDCP (DPE-PDCP) and diisopentyl ester of PDCP (DIPE-PDCP) belong to class I (negligible membrane retention and low permeation). Finally, quantitative structure – permeability and structure – retention relationships models were created in order to find quantitative relationships between physico-chemical properties of tested compounds and PAMPA membrane permeability/membrane retention parameters. Statistically the most reliable models were analysed and used for the design of new compounds for which favourable membrane permeability and retention can be expected.Supplementary material: [http://cherry.chem.bg.ac.rs/handle/123456789/3870]This is the peer-reviewed version of the following article: Tubić, B.; Dobričić, V.; Poljarević, J.; Savić, A.; Sabo, T.; Marković, B. Estimation of Passive Gastrointestinal Absorption and Membrane Retention Using PAMPA Test, Quantitative Structure-Permeability and Quantitative Structure-Retention Relationship Analyses of Ethylenediamine-N,N’-Di-2-(3-Cyclohexyl)Propanoic Acid and 1,3-Propanediamine-N,N’-Di-2-(3-Cyclohexyl)Propanoic Acid Derivatives. Journal of Pharmaceutical and Biomedical Analysis 2020, 184. [https://doi.org/10.1016/j.jpba.2020.113213

  • Estimation of passive gastrointestinal absorption and membrane retention using PAMPA test, quantitative structure-permeability and quantitative structure-retention relationship analyses of ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid and 1,
    Elsevier B.V., 2020
    Co-Authors: Tubić, Biljana K., Dobričić Vladimir, Poljarević Jelena, Savić Aleksandar, Sabo Tibor, Marković, Bojan D.
    Abstract:

    Passive gastrointestinal absorption and membrane retention of twelve esters of (S,S)-ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid (EDCP) and (S,S)-1,3-propanediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid (PDCP), as well as of these two non-esterified acids were estimated using PAMPA test. Artificial PAMPA membrane used in this study for the simulation of gastrointestinal barrier was solution of Egg Lecithin in dodecane (1 % w/v). All tested compounds belong to class III (high membrane retention and low permeation), whereas EDCP, dipentyl ester of PDCP (DPE-PDCP) and diisopentyl ester of PDCP (DIPE-PDCP) belong to class I (negligible membrane retention and low permeation). Finally, quantitative structure – permeability and structure – retention relationships models were created in order to find quantitative relationships between physico-chemical properties of tested compounds and PAMPA membrane permeability/membrane retention parameters. Statistically the most reliable models were analysed and used for the design of new compounds for which favourable membrane permeability and retention can be expected.Peer-reviewed manuscript: [http://cherry.chem.bg.ac.rs/handle/123456789/3869]Supplementary material: [http://cherry.chem.bg.ac.rs/handle/123456789/3870

  • Estimation of passive gastrointestinal absorption and membrane retention using PAMPA test, quantitative structure-permeability and quantitative structure-retention relationship analyses of ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid and 1,
    'Elsevier BV', 2020
    Co-Authors: Tubić Biljana, Dobričić Vladimir, Poljarević Jelena, Savić Aleksandar, Sabo Tibor, Marković Bojan
    Abstract:

    Passive gastrointestinal absorption and membrane retention of twelve esters of (S,S)-ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid (EDCP) and (S,S)-1,3-propanediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid (PDCP), as well as of these two non-esterified acids were estimated using PAMPA test. Artificial PAMPA membrane used in this study for the simulation of gastrointestinal barrier was solution of Egg Lecithin in dodecane (1 % w/v). All tested compounds belong to class III (high membrane retention and low permeation), whereas EDCP, dipentyl ester of PDCP (DPE-PDCP) and diisopentyl ester of PDCP (DIPE-PDCP) belong to class I (negligible membrane retention and low permeation). Finally, quantitative structure – permeability and structure – retention relationships models were created in order to find quantitative relationships between physico-chemical properties of tested compounds and PAMPA membrane permeability/membrane retention parameters. Statistically the most reliable models were analysed and used for the design of new compounds for which favourable membrane permeability and retention can be expected.Peer-reviewed manuscript: [http://farfar.pharmacy.bg.ac.rs/handle/123456789/3553

Savić Aleksandar - One of the best experts on this subject based on the ideXlab platform.

  • Estimation of passive gastrointestinal absorption and membrane retention using PAMPA test, quantitative structure-permeability and quantitative structure-retention relationship analyses of ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid and 1,
    'Elsevier BV', 2020
    Co-Authors: Tubić Biljana, Dobričić Vladimir, Poljarević Jelena, Savić Aleksandar, Sabo Tibor, Marković Bojan
    Abstract:

    Passive gastrointestinal absorption and membrane retention of twelve esters of (S,S)-ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid (EDCP) and (S,S)-1,3-propanediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid (PDCP), as well as of these two non-esterified acids were estimated using PAMPA test. Artificial PAMPA membrane used in this study for the simulation of gastrointestinal barrier was solution of Egg Lecithin in dodecane (1 % w/v). All tested compounds belong to class III (high membrane retention and low permeation), whereas EDCP, dipentyl ester of PDCP (DPE-PDCP) and diisopentyl ester of PDCP (DIPE-PDCP) belong to class I (negligible membrane retention and low permeation). Finally, quantitative structure – permeability and structure – retention relationships models were created in order to find quantitative relationships between physico-chemical properties of tested compounds and PAMPA membrane permeability/membrane retention parameters. Statistically the most reliable models were analysed and used for the design of new compounds for which favourable membrane permeability and retention can be expected.This is the peer-reviewed version of the following article: Tubić, B.; Dobričić, V.; Poljarević, J.; Savić, A.; Sabo, T.; Marković, B. Estimation of Passive Gastrointestinal Absorption and Membrane Retention Using PAMPA Test, Quantitative Structure-Permeability and Quantitative Structure-Retention Relationship Analyses of Ethylenediamine-N,N’-Di-2-(3-Cyclohexyl)Propanoic Acid and 1,3-Propanediamine-N,N’-Di-2-(3-Cyclohexyl)Propanoic Acid Derivatives. Journal of Pharmaceutical and Biomedical Analysis 2020, 184. [https://doi.org/10.1016/j.jpba.2020.113213

  • Estimation of passive gastrointestinal absorption and membrane retention using PAMPA test, quantitative structure-permeability and quantitative structure-retention relationship analyses of ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid and 1,
    Elsevier B.V., 2020
    Co-Authors: Tubić, Biljana K., Dobričić Vladimir, Poljarević Jelena, Savić Aleksandar, Sabo Tibor, Marković, Bojan D.
    Abstract:

    Passive gastrointestinal absorption and membrane retention of twelve esters of (S,S)-ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid (EDCP) and (S,S)-1,3-propanediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid (PDCP), as well as of these two non-esterified acids were estimated using PAMPA test. Artificial PAMPA membrane used in this study for the simulation of gastrointestinal barrier was solution of Egg Lecithin in dodecane (1 % w/v). All tested compounds belong to class III (high membrane retention and low permeation), whereas EDCP, dipentyl ester of PDCP (DPE-PDCP) and diisopentyl ester of PDCP (DIPE-PDCP) belong to class I (negligible membrane retention and low permeation). Finally, quantitative structure – permeability and structure – retention relationships models were created in order to find quantitative relationships between physico-chemical properties of tested compounds and PAMPA membrane permeability/membrane retention parameters. Statistically the most reliable models were analysed and used for the design of new compounds for which favourable membrane permeability and retention can be expected.Supplementary material: [http://cherry.chem.bg.ac.rs/handle/123456789/3870]This is the peer-reviewed version of the following article: Tubić, B.; Dobričić, V.; Poljarević, J.; Savić, A.; Sabo, T.; Marković, B. Estimation of Passive Gastrointestinal Absorption and Membrane Retention Using PAMPA Test, Quantitative Structure-Permeability and Quantitative Structure-Retention Relationship Analyses of Ethylenediamine-N,N’-Di-2-(3-Cyclohexyl)Propanoic Acid and 1,3-Propanediamine-N,N’-Di-2-(3-Cyclohexyl)Propanoic Acid Derivatives. Journal of Pharmaceutical and Biomedical Analysis 2020, 184. [https://doi.org/10.1016/j.jpba.2020.113213

  • Estimation of passive gastrointestinal absorption and membrane retention using PAMPA test, quantitative structure-permeability and quantitative structure-retention relationship analyses of ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid and 1,
    Elsevier B.V., 2020
    Co-Authors: Tubić, Biljana K., Dobričić Vladimir, Poljarević Jelena, Savić Aleksandar, Sabo Tibor, Marković, Bojan D.
    Abstract:

    Passive gastrointestinal absorption and membrane retention of twelve esters of (S,S)-ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid (EDCP) and (S,S)-1,3-propanediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid (PDCP), as well as of these two non-esterified acids were estimated using PAMPA test. Artificial PAMPA membrane used in this study for the simulation of gastrointestinal barrier was solution of Egg Lecithin in dodecane (1 % w/v). All tested compounds belong to class III (high membrane retention and low permeation), whereas EDCP, dipentyl ester of PDCP (DPE-PDCP) and diisopentyl ester of PDCP (DIPE-PDCP) belong to class I (negligible membrane retention and low permeation). Finally, quantitative structure – permeability and structure – retention relationships models were created in order to find quantitative relationships between physico-chemical properties of tested compounds and PAMPA membrane permeability/membrane retention parameters. Statistically the most reliable models were analysed and used for the design of new compounds for which favourable membrane permeability and retention can be expected.Peer-reviewed manuscript: [http://cherry.chem.bg.ac.rs/handle/123456789/3869]Supplementary material: [http://cherry.chem.bg.ac.rs/handle/123456789/3870

  • Estimation of passive gastrointestinal absorption and membrane retention using PAMPA test, quantitative structure-permeability and quantitative structure-retention relationship analyses of ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid and 1,
    'Elsevier BV', 2020
    Co-Authors: Tubić Biljana, Dobričić Vladimir, Poljarević Jelena, Savić Aleksandar, Sabo Tibor, Marković Bojan
    Abstract:

    Passive gastrointestinal absorption and membrane retention of twelve esters of (S,S)-ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid (EDCP) and (S,S)-1,3-propanediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid (PDCP), as well as of these two non-esterified acids were estimated using PAMPA test. Artificial PAMPA membrane used in this study for the simulation of gastrointestinal barrier was solution of Egg Lecithin in dodecane (1 % w/v). All tested compounds belong to class III (high membrane retention and low permeation), whereas EDCP, dipentyl ester of PDCP (DPE-PDCP) and diisopentyl ester of PDCP (DIPE-PDCP) belong to class I (negligible membrane retention and low permeation). Finally, quantitative structure – permeability and structure – retention relationships models were created in order to find quantitative relationships between physico-chemical properties of tested compounds and PAMPA membrane permeability/membrane retention parameters. Statistically the most reliable models were analysed and used for the design of new compounds for which favourable membrane permeability and retention can be expected.Peer-reviewed manuscript: [http://farfar.pharmacy.bg.ac.rs/handle/123456789/3553