Enhanced and Sustained Transdermal Delivery of Oxypurinol Using Thermosensitive Gel Combined with Polymeric Solid Microneedles DOI Creative Commons

Siti Nur Fatimah S. Mohamad,

Stephanie Stephanie,

Zulfiayu Sapiun

et al.

ACS Omega, Journal Year: 2024, Volume and Issue: 10(4), P. 3500 - 3510

Published: Dec. 20, 2024

Gout is a pathological condition caused by monosodium urate crystal deposition in tissues. Allopurinol, the first-line therapy, inhibits xanthine oxidase but may be ineffective due to reduced conversion oxypurinol (OXY). Current delivery routes for OXY, including oral and intravenous routes, have drawbacks such as poor solubility patient discomfort. This study developed system integrating thermosensitive gel (TRG) containing OXY with polymeric solid microneedles (PSMNs). Molecular docking demonstrated high-affinity binding interactions between Pluronic (−2.5). The TRG, formulated F127 F68, was assessed gelation temperature, pH, spreadability, bioadhesive strength. PSMN, made from poly(vinyl alcohol) polyvinylpyrrolidone K-30 citric acid, evaluated mechanical strength skin penetration. In vitro hemolysis activity, drug release, ex vivo permeation studies were conducted. results showed stable an affinity of −2.5 ligands Pluronic. TRG formulation exhibited promising characteristics transdermal delivery. PSMN good able penetrate up 504 μm. Hemolysis testing that TSG safe ratio less than 5%. release high 2.24 ± 0.26 mg highest concentration displaying sustained profile. Ex significant difference (p < 0.05) without combination. increased 79–81% compared PSMN. successfully combined enhance OXY. These suggest new route delivery, potentially offering more efficient user-friendly treatment chronic gout. Further are needed evaluate efficacy, pharmacokinetics, pharmacodynamics, interactions, toxicity further clinical applications.

Language: Английский

Development of Pluronic-Based Micelles from Palm Oil Bioactive Compounds Incorporated by a Dissolvable Microarray Patch to Enhance the Efficacy of Atopic Dermatitis Therapy DOI

Khusnul Humayatul Jannah,

Christopher Kosasi Ko,

Felicia Virginia Thios

et al.

Molecular Pharmaceutics, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 13, 2025

The high content of vitamin E, including tocopherols and tocotrienols (TCF-TTE), in palm oil (Elaeis guineensis) has made it a promising candidate for the alternative treatment atopic dermatitis (AD). However, limited solubility TCF-TTE restricted its therapeutic efficacy. In this study, pluronic-based micelles (MCs) encapsulating oil-derived were formulated with dissolvable microarray patch-micelles (DMP-MC) using carboxymethyl cellulose (CMC) synthesized from empty fruit bunches to optimize delivery AD. MC was prepared direct dissolution method Pluronic F68 F127. results showed that increased TCF-TTE, which further confirmed by an vitro study where 90.23 ± 2.07% TCF 4.56 1.36% TTE released compared unencapsulated extract. Furthermore, CMC biopolymers integrated into DMP-MC polyvinylpyrrolidone (PVP) exhibited favorable physical properties, such as mechanical strength penetration ability. also better platform lower permeation, indicating higher retention localized effects on AD skin than cream-MC. Additionally, dermatokinetic profile parameters significant improvement. mean residence time (MRT) parameter indicated retained longer times 19.28 0.02 h 20.68 0.01 h. Moreover, vivo revealed could relieve symptoms more rapidly oral doses cream-MC, proved be efficient. no tissue destruction (granulation fibrosis) rats treated seventh day. Therefore, successfully developed formula formulation CMC, potentially improve AD's

Language: Английский

Citations

1
Fucoidan and its derivatives: From extraction to cutting-edge biomedical applications DOI
Mohamed Farid Abbas,

Dhuha K Karim,

Huda Raad Kareem

et al.

Carbohydrate Polymers, Journal Year: 2025, Volume and Issue: 357, P. 123468 - 123468

Published: March 1, 2025

Language: Английский

Citations

1
Development of thermosensitive mucoadhesive gel incorporated lipid microspheres of donepezil for enhanced nose-to-brain delivery DOI

Rachmatya W. Tuna,

Nurafni Annisa Achmad,

Irfan Kurniawan

et al.

Journal of Biomaterials Science Polymer Edition, Journal Year: 2025, Volume and Issue: unknown, P. 1 - 28

Published: April 22, 2025

Alzheimer's disease (ALZ) is a chronic that affects the brain neurons leading to dementia. Donepezil (DPZ), first-line treatment for ALZ potent symptomatic therapeutic agent. However, oral and transdermal route represents non-targeted delivery, causing various adverse effects. This study presents successful incorporation of DPZ-loaded lipid microsphere (DPZ-LM) system into thermosensitive-mucoadhesive gel (TMG), thereby enhancing delivery DPZ through nose-to-brain route. To optimize formulations, several evaluations were conducted, resulting in an optimized formulation LM using Compritol® exhibited particle size 8.75 µm, 98.44% entrapped, 93.40% loaded with sustained release manner vitro studies. The TMG-DPZ-LM was prepared Pluronic® F127 F68, as gelling agents, addition sodium alginate, mucoadhesive polymer. Following TMG-DPZ-LM, excellent physicochemical properties effective nasal ex vivo permeation has found 88.58 ± 12.53 µg/cm2 retention studies mean concentration 0.0077 mg porcine mucosa. pharmacokinetic demonstrated administration via resulted significant (p < 0.05) increase Cmax, 207.24 5.16 µg/cm3 significantly different profile compared other formulation. developed this considered have improved its efficacy ALZ.

Language: Английский

Citations

0
Controlled release of deferiprone using iron-responsive nanoparticles integrated with dissolving microneedle for novel alternative treatments of β-thalassemia major DOI

Muh. Taufik Hidayat,

Sitti Nur Khadijah Maharani,

Indianty Dwi Ramadhany

et al.

European Journal of Pharmaceutics and Biopharmaceutics, Journal Year: 2025, Volume and Issue: unknown, P. 114702 - 114702

Published: March 1, 2025

Language: Английский

Citations

0
Hispidulin-rich fraction of Clerodendrum fragrans Wild. (Sesewanua) dissolving microneedle as antithrombosis candidate: A proof of concept study DOI
Zulfiayu Sapiun, Arlan K. Imran,

Siti Nur Fatimah S. Mohamad

et al.

International Journal of Pharmaceutics, Journal Year: 2024, Volume and Issue: unknown, P. 124766 - 124766

Published: Sept. 1, 2024

Language: Английский

Citations

2
Iron-Responsive Nanoparticle-Loaded Bilayer Dissolving Microneedles for Selective and Controlled Transdermal Delivery of Deferasirox in β-Thalassemia Major Treatment DOI
Andi Dian Permana,

Sitti Nurkhadijah Maharani,

Anugerah Yaumil Ramadhani Aziz

et al.

Colloids and Surfaces B Biointerfaces, Journal Year: 2024, Volume and Issue: 247, P. 114416 - 114416

Published: Nov. 30, 2024

Language: Английский

Citations

0
Development of three-layer microneedle system for controlled and sustained release of Levonorgestrel: A pioneering approach to long-term contraceptive delivery DOI
Andi Dian Permana,

Anugerah Yaumil Ramadhani Aziz,

Nur Rezky Aulia Ilyas

et al.

International Journal of Pharmaceutics, Journal Year: 2024, Volume and Issue: unknown, P. 125085 - 125085

Published: Dec. 1, 2024

Language: Английский

Citations

0
Enhanced and Sustained Transdermal Delivery of Oxypurinol Using Thermosensitive Gel Combined with Polymeric Solid Microneedles DOI Creative Commons

Siti Nur Fatimah S. Mohamad,

Stephanie Stephanie,

Zulfiayu Sapiun

et al.

ACS Omega, Journal Year: 2024, Volume and Issue: 10(4), P. 3500 - 3510

Published: Dec. 20, 2024

Gout is a pathological condition caused by monosodium urate crystal deposition in tissues. Allopurinol, the first-line therapy, inhibits xanthine oxidase but may be ineffective due to reduced conversion oxypurinol (OXY). Current delivery routes for OXY, including oral and intravenous routes, have drawbacks such as poor solubility patient discomfort. This study developed system integrating thermosensitive gel (TRG) containing OXY with polymeric solid microneedles (PSMNs). Molecular docking demonstrated high-affinity binding interactions between Pluronic (−2.5). The TRG, formulated F127 F68, was assessed gelation temperature, pH, spreadability, bioadhesive strength. PSMN, made from poly(vinyl alcohol) polyvinylpyrrolidone K-30 citric acid, evaluated mechanical strength skin penetration. In vitro hemolysis activity, drug release, ex vivo permeation studies were conducted. results showed stable an affinity of −2.5 ligands Pluronic. TRG formulation exhibited promising characteristics transdermal delivery. PSMN good able penetrate up 504 μm. Hemolysis testing that TSG safe ratio less than 5%. release high 2.24 ± 0.26 mg highest concentration displaying sustained profile. Ex significant difference (p < 0.05) without combination. increased 79–81% compared PSMN. successfully combined enhance OXY. These suggest new route delivery, potentially offering more efficient user-friendly treatment chronic gout. Further are needed evaluate efficacy, pharmacokinetics, pharmacodynamics, interactions, toxicity further clinical applications.

Language: Английский

Citations

0