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Formulation Development and Characterization of pH Responsive Polymeric Nano-Pharmaceuticals for Targeted Delivery of Anti-Cancer Drug (Methotrexate)

Oral administration of pH sensitive/stimuli responsive nanoparticles are gaining importance because of the limited side effects, minimum dose and controlled drug release. The objective of this study was to develop and evaluate pH sensitive polymeric nanoparticles for methotrexate with the aim to max...

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Autores principales: Ullah, Farhad, Iqbal, Zafar, Khan, Amjad, Khan, Saeed Ahmad, Ahmad, Lateef, Alotaibi, Amal, Ullah, Riaz, Shafique, Muhammad
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Frontiers Media S.A. 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9291017/
https://www.ncbi.nlm.nih.gov/pubmed/35860013
http://dx.doi.org/10.3389/fphar.2022.911771
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author Ullah, Farhad
Iqbal, Zafar
Khan, Amjad
Khan, Saeed Ahmad
Ahmad, Lateef
Alotaibi, Amal
Ullah, Riaz
Shafique, Muhammad
author_facet Ullah, Farhad
Iqbal, Zafar
Khan, Amjad
Khan, Saeed Ahmad
Ahmad, Lateef
Alotaibi, Amal
Ullah, Riaz
Shafique, Muhammad
author_sort Ullah, Farhad
collection PubMed
description Oral administration of pH sensitive/stimuli responsive nanoparticles are gaining importance because of the limited side effects, minimum dose and controlled drug release. The objective of this study was to develop and evaluate pH sensitive polymeric nanoparticles for methotrexate with the aim to maximize the drug release at target site. In the presented study, pH sensitive polymeric nanoparticles of methotrexate were developed through modified solvent evaporation technique using polymer Eudragit S100. Different process parameters like drug to polymer ratio, speed of sonication, concentration of surfactant and time of sonication were optimized by evaluating their effects on particle size, PDI, zeta potential, entrapment/encapsulation efficiency. The developed formulations were evaluated for their size, polydispersity (PDI), zeta potential, encapsulation efficiency, XRD, scanning electron microscopy, in-vitro drug release and stability studies. Best results were obtained with poloxamer-407 and PVA and were selected as surfactants. Physicochemical characterization of the developed formulations showed that the particle size lies in the range 165.7 ± 1.85–330.4 ± 4.19, PDI 0.119 ± 0.02–0.235 ± 0.008, zeta potential −0.163 ± 0.11–−5.64 ± 0.36 mV, and encapsulation efficiency more than 61%. The results of scanning electron microscopy revealed that nanoparticles have regular geometry with spherical shape. Initially the drug release occur through diffusion followed by erosion. The present studies showed that MTX-ES100 nanoparticles prepared during this study have the desired physicochemical properties, surface morphology and release characteristics used to target the desired organs.
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spelling pubmed-92910172022-07-19 Formulation Development and Characterization of pH Responsive Polymeric Nano-Pharmaceuticals for Targeted Delivery of Anti-Cancer Drug (Methotrexate) Ullah, Farhad Iqbal, Zafar Khan, Amjad Khan, Saeed Ahmad Ahmad, Lateef Alotaibi, Amal Ullah, Riaz Shafique, Muhammad Front Pharmacol Pharmacology Oral administration of pH sensitive/stimuli responsive nanoparticles are gaining importance because of the limited side effects, minimum dose and controlled drug release. The objective of this study was to develop and evaluate pH sensitive polymeric nanoparticles for methotrexate with the aim to maximize the drug release at target site. In the presented study, pH sensitive polymeric nanoparticles of methotrexate were developed through modified solvent evaporation technique using polymer Eudragit S100. Different process parameters like drug to polymer ratio, speed of sonication, concentration of surfactant and time of sonication were optimized by evaluating their effects on particle size, PDI, zeta potential, entrapment/encapsulation efficiency. The developed formulations were evaluated for their size, polydispersity (PDI), zeta potential, encapsulation efficiency, XRD, scanning electron microscopy, in-vitro drug release and stability studies. Best results were obtained with poloxamer-407 and PVA and were selected as surfactants. Physicochemical characterization of the developed formulations showed that the particle size lies in the range 165.7 ± 1.85–330.4 ± 4.19, PDI 0.119 ± 0.02–0.235 ± 0.008, zeta potential −0.163 ± 0.11–−5.64 ± 0.36 mV, and encapsulation efficiency more than 61%. The results of scanning electron microscopy revealed that nanoparticles have regular geometry with spherical shape. Initially the drug release occur through diffusion followed by erosion. The present studies showed that MTX-ES100 nanoparticles prepared during this study have the desired physicochemical properties, surface morphology and release characteristics used to target the desired organs. Frontiers Media S.A. 2022-06-30 /pmc/articles/PMC9291017/ /pubmed/35860013 http://dx.doi.org/10.3389/fphar.2022.911771 Text en Copyright © 2022 Ullah, Iqbal, Khan, Khan, Ahmad, Alotaibi, Ullah and Shafique. https://creativecommons.org/licenses/by/4.0/This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
spellingShingle Pharmacology
Ullah, Farhad
Iqbal, Zafar
Khan, Amjad
Khan, Saeed Ahmad
Ahmad, Lateef
Alotaibi, Amal
Ullah, Riaz
Shafique, Muhammad
Formulation Development and Characterization of pH Responsive Polymeric Nano-Pharmaceuticals for Targeted Delivery of Anti-Cancer Drug (Methotrexate)
title Formulation Development and Characterization of pH Responsive Polymeric Nano-Pharmaceuticals for Targeted Delivery of Anti-Cancer Drug (Methotrexate)
title_full Formulation Development and Characterization of pH Responsive Polymeric Nano-Pharmaceuticals for Targeted Delivery of Anti-Cancer Drug (Methotrexate)
title_fullStr Formulation Development and Characterization of pH Responsive Polymeric Nano-Pharmaceuticals for Targeted Delivery of Anti-Cancer Drug (Methotrexate)
title_full_unstemmed Formulation Development and Characterization of pH Responsive Polymeric Nano-Pharmaceuticals for Targeted Delivery of Anti-Cancer Drug (Methotrexate)
title_short Formulation Development and Characterization of pH Responsive Polymeric Nano-Pharmaceuticals for Targeted Delivery of Anti-Cancer Drug (Methotrexate)
title_sort formulation development and characterization of ph responsive polymeric nano-pharmaceuticals for targeted delivery of anti-cancer drug (methotrexate)
topic Pharmacology
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9291017/
https://www.ncbi.nlm.nih.gov/pubmed/35860013
http://dx.doi.org/10.3389/fphar.2022.911771
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