Cargando…

Biodegradable Polymers-Based Smart Nanocrystals for Loxoprofen Delivery with Enhanced Solubility: Design, Fabrication and Physical Characterizations

Nanocrystals are carrier-free, submicron-sized, colloidal drug delivery systems with particle sizes in the mean nanometer range. Nanocrystals have high bioavailability and fast absorption because of their high dissolution velocity and enhanced adhesiveness to cell membranes. Loxoprofen, a nonsteroid...

Descripción completa

Detalles Bibliográficos
Autores principales: Khan, Barkat Ali, Khalid, Hina, Khan, Muhammad Khalid, Hosny, Khaled M., Khan, Shahzeb, Rizg, Waleed Y., Safhi, Awaji Y., Halwani, Abdulrahman A., Almehmady, Alshaimaa M., Menaa, Farid
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9460905/
https://www.ncbi.nlm.nih.gov/pubmed/36080539
http://dx.doi.org/10.3390/polym14173464
_version_ 1784786861591363584
author Khan, Barkat Ali
Khalid, Hina
Khan, Muhammad Khalid
Hosny, Khaled M.
Khan, Shahzeb
Rizg, Waleed Y.
Safhi, Awaji Y.
Halwani, Abdulrahman A.
Almehmady, Alshaimaa M.
Menaa, Farid
author_facet Khan, Barkat Ali
Khalid, Hina
Khan, Muhammad Khalid
Hosny, Khaled M.
Khan, Shahzeb
Rizg, Waleed Y.
Safhi, Awaji Y.
Halwani, Abdulrahman A.
Almehmady, Alshaimaa M.
Menaa, Farid
author_sort Khan, Barkat Ali
collection PubMed
description Nanocrystals are carrier-free, submicron-sized, colloidal drug delivery systems with particle sizes in the mean nanometer range. Nanocrystals have high bioavailability and fast absorption because of their high dissolution velocity and enhanced adhesiveness to cell membranes. Loxoprofen, a nonsteroidal anti-inflammatory drug belonging to the Biopharmaceutical Classification System (BCS) II drug class, was selected as the model drug. The aim of this study was to formulate nanocrystals of loxoprofen. A total of 12 formulations (F1 to F12) were prepared. An antisolvent technique was used to determine the effects of various stabilizers and processing conditions on the optimization of formulations. The various stabilizers used were hydroxypropyl methylcellulose (0.5%), polyvinylpyrrolidone (0.5%), and sodium lauryl sulfate (0.1%). The various characterizations conducted for this research included stability studies at 25 °C and 4 °C, scanning electron microscopy, transmission electron microscopy (TEM), X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), zeta potentials, polydispersity indexes, and dissolution studies. F10 was the optimized formulation that showed stability at room temperature, as well as at a refrigerated temperature, for 30 days. A high dissolution rate (100% within the first 10 min) was shown by comparative dissolution studies of nano-suspensions with the micro-suspension and raw loxoprofen. F10 formulation had a non-porous and crystalline morphology on evaluation by TEM and XRPD, respectively, and the average particle size was 300 ± 0.3 nm as confirmed by TEM. DSC recorded a reduction in the melting point (180 °C processed and 200 °C unprocessed melting points). The dissolution rate and solubility of the formulated loxoprofen nanocrystals were significantly enhanced. It can be concluded that selecting suitable stabilizers (i.e., polymers and surfactants) can produce stable nanocrystals, and this can potentially lead to a scaling up of the process for commercialization.
format Online
Article
Text
id pubmed-9460905
institution National Center for Biotechnology Information
language English
publishDate 2022
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-94609052022-09-10 Biodegradable Polymers-Based Smart Nanocrystals for Loxoprofen Delivery with Enhanced Solubility: Design, Fabrication and Physical Characterizations Khan, Barkat Ali Khalid, Hina Khan, Muhammad Khalid Hosny, Khaled M. Khan, Shahzeb Rizg, Waleed Y. Safhi, Awaji Y. Halwani, Abdulrahman A. Almehmady, Alshaimaa M. Menaa, Farid Polymers (Basel) Article Nanocrystals are carrier-free, submicron-sized, colloidal drug delivery systems with particle sizes in the mean nanometer range. Nanocrystals have high bioavailability and fast absorption because of their high dissolution velocity and enhanced adhesiveness to cell membranes. Loxoprofen, a nonsteroidal anti-inflammatory drug belonging to the Biopharmaceutical Classification System (BCS) II drug class, was selected as the model drug. The aim of this study was to formulate nanocrystals of loxoprofen. A total of 12 formulations (F1 to F12) were prepared. An antisolvent technique was used to determine the effects of various stabilizers and processing conditions on the optimization of formulations. The various stabilizers used were hydroxypropyl methylcellulose (0.5%), polyvinylpyrrolidone (0.5%), and sodium lauryl sulfate (0.1%). The various characterizations conducted for this research included stability studies at 25 °C and 4 °C, scanning electron microscopy, transmission electron microscopy (TEM), X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), zeta potentials, polydispersity indexes, and dissolution studies. F10 was the optimized formulation that showed stability at room temperature, as well as at a refrigerated temperature, for 30 days. A high dissolution rate (100% within the first 10 min) was shown by comparative dissolution studies of nano-suspensions with the micro-suspension and raw loxoprofen. F10 formulation had a non-porous and crystalline morphology on evaluation by TEM and XRPD, respectively, and the average particle size was 300 ± 0.3 nm as confirmed by TEM. DSC recorded a reduction in the melting point (180 °C processed and 200 °C unprocessed melting points). The dissolution rate and solubility of the formulated loxoprofen nanocrystals were significantly enhanced. It can be concluded that selecting suitable stabilizers (i.e., polymers and surfactants) can produce stable nanocrystals, and this can potentially lead to a scaling up of the process for commercialization. MDPI 2022-08-25 /pmc/articles/PMC9460905/ /pubmed/36080539 http://dx.doi.org/10.3390/polym14173464 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Khan, Barkat Ali
Khalid, Hina
Khan, Muhammad Khalid
Hosny, Khaled M.
Khan, Shahzeb
Rizg, Waleed Y.
Safhi, Awaji Y.
Halwani, Abdulrahman A.
Almehmady, Alshaimaa M.
Menaa, Farid
Biodegradable Polymers-Based Smart Nanocrystals for Loxoprofen Delivery with Enhanced Solubility: Design, Fabrication and Physical Characterizations
title Biodegradable Polymers-Based Smart Nanocrystals for Loxoprofen Delivery with Enhanced Solubility: Design, Fabrication and Physical Characterizations
title_full Biodegradable Polymers-Based Smart Nanocrystals for Loxoprofen Delivery with Enhanced Solubility: Design, Fabrication and Physical Characterizations
title_fullStr Biodegradable Polymers-Based Smart Nanocrystals for Loxoprofen Delivery with Enhanced Solubility: Design, Fabrication and Physical Characterizations
title_full_unstemmed Biodegradable Polymers-Based Smart Nanocrystals for Loxoprofen Delivery with Enhanced Solubility: Design, Fabrication and Physical Characterizations
title_short Biodegradable Polymers-Based Smart Nanocrystals for Loxoprofen Delivery with Enhanced Solubility: Design, Fabrication and Physical Characterizations
title_sort biodegradable polymers-based smart nanocrystals for loxoprofen delivery with enhanced solubility: design, fabrication and physical characterizations
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9460905/
https://www.ncbi.nlm.nih.gov/pubmed/36080539
http://dx.doi.org/10.3390/polym14173464
work_keys_str_mv AT khanbarkatali biodegradablepolymersbasedsmartnanocrystalsforloxoprofendeliverywithenhancedsolubilitydesignfabricationandphysicalcharacterizations
AT khalidhina biodegradablepolymersbasedsmartnanocrystalsforloxoprofendeliverywithenhancedsolubilitydesignfabricationandphysicalcharacterizations
AT khanmuhammadkhalid biodegradablepolymersbasedsmartnanocrystalsforloxoprofendeliverywithenhancedsolubilitydesignfabricationandphysicalcharacterizations
AT hosnykhaledm biodegradablepolymersbasedsmartnanocrystalsforloxoprofendeliverywithenhancedsolubilitydesignfabricationandphysicalcharacterizations
AT khanshahzeb biodegradablepolymersbasedsmartnanocrystalsforloxoprofendeliverywithenhancedsolubilitydesignfabricationandphysicalcharacterizations
AT rizgwaleedy biodegradablepolymersbasedsmartnanocrystalsforloxoprofendeliverywithenhancedsolubilitydesignfabricationandphysicalcharacterizations
AT safhiawajiy biodegradablepolymersbasedsmartnanocrystalsforloxoprofendeliverywithenhancedsolubilitydesignfabricationandphysicalcharacterizations
AT halwaniabdulrahmana biodegradablepolymersbasedsmartnanocrystalsforloxoprofendeliverywithenhancedsolubilitydesignfabricationandphysicalcharacterizations
AT almehmadyalshaimaam biodegradablepolymersbasedsmartnanocrystalsforloxoprofendeliverywithenhancedsolubilitydesignfabricationandphysicalcharacterizations
AT menaafarid biodegradablepolymersbasedsmartnanocrystalsforloxoprofendeliverywithenhancedsolubilitydesignfabricationandphysicalcharacterizations