Drug Granulation

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Mariadolores Veiga - One of the best experts on this subject based on the ideXlab platform.

  • improvement of tenofovir vaginal release from hydrophilic matrices through Drug Granulation with hydrophobic polymers
    European Journal of Pharmaceutical Sciences, 2018
    Co-Authors: Fernando Notarioperez, Araceli Martinillana, Raul Cazorlaluna, Roberto Ruizcaro, J Pena, Mariadolores Veiga
    Abstract:

    Abstract Sustained-release vaginal microbicides hold out great hope for the prevention of sexual transmission of HIV from men to women. Tenofovir (TFV) –an antiretroviral Drug– sustained-release vaginal compacts combining two release control systems (by Drug-loading granules with hydrophobic polymers and incorporating them in a hydrophilic matrix) are proposed in this work as a possible microbicide. The polymers used for the Drug granules are Eudragit® RS (ERS), an acrylic derivative, and Zein, a maize protein. The hydrophilic matrix is composed of a mixture of hydroxypropylmethyl cellulose (HPMC) and chitosan (CH). The thermal, microscopic, spectrophotometric and X-ray diffraction analysis showed that the Drug was not altered during the Granulation process. Studies of TFV release, swelling and ex vivo mucoadhesion were subsequently performed on simulated vaginal fluid. The formulation whereby TFV is granulated using twice its weight in ERS, and then including these granules in a matrix in which the CH predominates over HPMC, allows the sustained release of TFV for 144 h, mucoadhesion to the vaginal mucosa for 150 h and a moderate swelling, making it the most suitable formulation of all those studied. These compacts would therefore offer women protection against the sexual acquisition of HIV.

Fernando Notarioperez - One of the best experts on this subject based on the ideXlab platform.

  • improvement of tenofovir vaginal release from hydrophilic matrices through Drug Granulation with hydrophobic polymers
    European Journal of Pharmaceutical Sciences, 2018
    Co-Authors: Fernando Notarioperez, Araceli Martinillana, Raul Cazorlaluna, Roberto Ruizcaro, J Pena, Mariadolores Veiga
    Abstract:

    Abstract Sustained-release vaginal microbicides hold out great hope for the prevention of sexual transmission of HIV from men to women. Tenofovir (TFV) –an antiretroviral Drug– sustained-release vaginal compacts combining two release control systems (by Drug-loading granules with hydrophobic polymers and incorporating them in a hydrophilic matrix) are proposed in this work as a possible microbicide. The polymers used for the Drug granules are Eudragit® RS (ERS), an acrylic derivative, and Zein, a maize protein. The hydrophilic matrix is composed of a mixture of hydroxypropylmethyl cellulose (HPMC) and chitosan (CH). The thermal, microscopic, spectrophotometric and X-ray diffraction analysis showed that the Drug was not altered during the Granulation process. Studies of TFV release, swelling and ex vivo mucoadhesion were subsequently performed on simulated vaginal fluid. The formulation whereby TFV is granulated using twice its weight in ERS, and then including these granules in a matrix in which the CH predominates over HPMC, allows the sustained release of TFV for 144 h, mucoadhesion to the vaginal mucosa for 150 h and a moderate swelling, making it the most suitable formulation of all those studied. These compacts would therefore offer women protection against the sexual acquisition of HIV.

Araceli Martinillana - One of the best experts on this subject based on the ideXlab platform.

  • improvement of tenofovir vaginal release from hydrophilic matrices through Drug Granulation with hydrophobic polymers
    European Journal of Pharmaceutical Sciences, 2018
    Co-Authors: Fernando Notarioperez, Araceli Martinillana, Raul Cazorlaluna, Roberto Ruizcaro, J Pena, Mariadolores Veiga
    Abstract:

    Abstract Sustained-release vaginal microbicides hold out great hope for the prevention of sexual transmission of HIV from men to women. Tenofovir (TFV) –an antiretroviral Drug– sustained-release vaginal compacts combining two release control systems (by Drug-loading granules with hydrophobic polymers and incorporating them in a hydrophilic matrix) are proposed in this work as a possible microbicide. The polymers used for the Drug granules are Eudragit® RS (ERS), an acrylic derivative, and Zein, a maize protein. The hydrophilic matrix is composed of a mixture of hydroxypropylmethyl cellulose (HPMC) and chitosan (CH). The thermal, microscopic, spectrophotometric and X-ray diffraction analysis showed that the Drug was not altered during the Granulation process. Studies of TFV release, swelling and ex vivo mucoadhesion were subsequently performed on simulated vaginal fluid. The formulation whereby TFV is granulated using twice its weight in ERS, and then including these granules in a matrix in which the CH predominates over HPMC, allows the sustained release of TFV for 144 h, mucoadhesion to the vaginal mucosa for 150 h and a moderate swelling, making it the most suitable formulation of all those studied. These compacts would therefore offer women protection against the sexual acquisition of HIV.

Raul Cazorlaluna - One of the best experts on this subject based on the ideXlab platform.

  • improvement of tenofovir vaginal release from hydrophilic matrices through Drug Granulation with hydrophobic polymers
    European Journal of Pharmaceutical Sciences, 2018
    Co-Authors: Fernando Notarioperez, Araceli Martinillana, Raul Cazorlaluna, Roberto Ruizcaro, J Pena, Mariadolores Veiga
    Abstract:

    Abstract Sustained-release vaginal microbicides hold out great hope for the prevention of sexual transmission of HIV from men to women. Tenofovir (TFV) –an antiretroviral Drug– sustained-release vaginal compacts combining two release control systems (by Drug-loading granules with hydrophobic polymers and incorporating them in a hydrophilic matrix) are proposed in this work as a possible microbicide. The polymers used for the Drug granules are Eudragit® RS (ERS), an acrylic derivative, and Zein, a maize protein. The hydrophilic matrix is composed of a mixture of hydroxypropylmethyl cellulose (HPMC) and chitosan (CH). The thermal, microscopic, spectrophotometric and X-ray diffraction analysis showed that the Drug was not altered during the Granulation process. Studies of TFV release, swelling and ex vivo mucoadhesion were subsequently performed on simulated vaginal fluid. The formulation whereby TFV is granulated using twice its weight in ERS, and then including these granules in a matrix in which the CH predominates over HPMC, allows the sustained release of TFV for 144 h, mucoadhesion to the vaginal mucosa for 150 h and a moderate swelling, making it the most suitable formulation of all those studied. These compacts would therefore offer women protection against the sexual acquisition of HIV.

Roberto Ruizcaro - One of the best experts on this subject based on the ideXlab platform.

  • improvement of tenofovir vaginal release from hydrophilic matrices through Drug Granulation with hydrophobic polymers
    European Journal of Pharmaceutical Sciences, 2018
    Co-Authors: Fernando Notarioperez, Araceli Martinillana, Raul Cazorlaluna, Roberto Ruizcaro, J Pena, Mariadolores Veiga
    Abstract:

    Abstract Sustained-release vaginal microbicides hold out great hope for the prevention of sexual transmission of HIV from men to women. Tenofovir (TFV) –an antiretroviral Drug– sustained-release vaginal compacts combining two release control systems (by Drug-loading granules with hydrophobic polymers and incorporating them in a hydrophilic matrix) are proposed in this work as a possible microbicide. The polymers used for the Drug granules are Eudragit® RS (ERS), an acrylic derivative, and Zein, a maize protein. The hydrophilic matrix is composed of a mixture of hydroxypropylmethyl cellulose (HPMC) and chitosan (CH). The thermal, microscopic, spectrophotometric and X-ray diffraction analysis showed that the Drug was not altered during the Granulation process. Studies of TFV release, swelling and ex vivo mucoadhesion were subsequently performed on simulated vaginal fluid. The formulation whereby TFV is granulated using twice its weight in ERS, and then including these granules in a matrix in which the CH predominates over HPMC, allows the sustained release of TFV for 144 h, mucoadhesion to the vaginal mucosa for 150 h and a moderate swelling, making it the most suitable formulation of all those studied. These compacts would therefore offer women protection against the sexual acquisition of HIV.