Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Development and Evaluation of Apocynin Loaded pH-sensitive Nanoparticle Based Hydrogel for the Management of Rheumatoid Arthritis

Rasikha Akbar
,
Dildar Khan
,
Muhammad Bilal Sabir
,
Irfan Shaukat
,
Irfa Basharat Rajpoot
,
Asim Ur Rehman
,
Naz Dilawar
,
Shefaat Ullah Shah
,
Asif Nawaz
ORCID logo ,
Faiqa Falak Naz
,
Saima Mehmood
,
Hafiz Muhammad Basit
,
Suliman Yousef Alomar
* ,
Kifayat Ullah Shah
* ORCID logo
Version 1 : Received: 22 May 2023 / Approved: 23 May 2023 / Online: 23 May 2023 (07:51:12 CEST)

How to cite: Akbar, R.; Khan, D.; Sabir, M.B.; Shaukat, I.; Rajpoot, I.B.; Rehman, A.U.; Dilawar, N.; Shah, S.U.; Nawaz, A.; Naz, F.F.; Mehmood, S.; Basit, H.M.; Alomar, S.Y.; Shah, K.U. Development and Evaluation of Apocynin Loaded pH-sensitive Nanoparticle Based Hydrogel for the Management of Rheumatoid Arthritis. Preprints 2023, 2023051605. https://doi.org/10.20944/preprints202305.1605.v1 Akbar, R.; Khan, D.; Sabir, M.B.; Shaukat, I.; Rajpoot, I.B.; Rehman, A.U.; Dilawar, N.; Shah, S.U.; Nawaz, A.; Naz, F.F.; Mehmood, S.; Basit, H.M.; Alomar, S.Y.; Shah, K.U. Development and Evaluation of Apocynin Loaded pH-sensitive Nanoparticle Based Hydrogel for the Management of Rheumatoid Arthritis. Preprints 2023, 2023051605. https://doi.org/10.20944/preprints202305.1605.v1

Abstract

The aim of the current study was to develop and evaluate the therapeutic potential of apocynin (APO) loaded pH-sensitive nanoparticles (NPs) based transdermal hydrogel for management of rheumatoid arthritis (RA). Slightly modified nanoprecipitation technique was used for preparation of polymeric nanoparticles. Optimization was done through design expert software. Optimized APO-NPs were loaded into carbopol-934 based hydrogel as final dosage form and further studied for physicochemical properties. Optimized APO-NPs formulation had a minimum particle size 63.44 nm, polydisperibility index 0.161, and zeta potential -15mV with a maximum encapsulation efficiency of 89%. In-vitro and ex-vivo studies of APO-NPs based hydrogel was performed at pH 5.5 (pH of normal skin) and 6.8 (pH of inflammed joint) showed a pH-responsive sustained drug release and increased penetration in comparison to free APO based hydrogel. The stability studies of APO-NPs based hydrogel were done to strengthen the potential use of the prepared formulation through transdermal route. Assessment and therapeutic efficacy of the prepared pH-sensitive nanocarriers system was evaluated in chronic inflammatory RA mice model. Parameters associated with chronic inflammation were investigated including behavioral changes and histopathological, and radiological x-rays images of joints of mice paws. In-vivo study depicts improvement in behavioral parameter, decline in synovial hyperplasia and bone structure restoration. In conclusion, APO loaded pH-sensitive NPs based transdermal is a promising carrier system that can effectively manage RA.

Keywords

pH sensitive Polymer; Methacrylate Polymers; Eudragit L100; Polymeric nanoparticles; Apocynin; Rheumatoid arthritis; Carbopol-934 based Hydrogel; Transdermal Drug Delivery System

Subject

Medicine and Pharmacology, Pharmacy

Copyright: This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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