Stability and Controlled Release of Amoxicillin Trihydrate in Novel Biopolymer Matrices
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Abstract
Amoxicillin trihydrate is a widely prescribed β-lactam antibiotic, suffers from chemical instability that limits its therapeutic efficacy and shelf life. This study investigates the formulation of controlled-release systems using locally sourced biopolymers in England, specifically alginate, chitosan, and pectin, to enhance drug stability and optimize release profiles. Microspheres were prepared via ionic gelation with varying polymer-to-drug ratios and characterized for particle morphology, thermal properties, crystallinity, and drug–polymer compatibility using SEM, DSC, XRD, and FTIR. Accelerated stability studies were conducted at 40°C and 75% relative humidity for 90 days, while in vitro release was assessed in simulated gastrointestinal fluids at pH 1.2 and 6.8. The results indicated that alginate–chitosan matrices provided superior encapsulation efficiency (>85%), structural integrity, and prolonged stability, reducing the degradation rate by up to fourfold compared to unencapsulated drug. Pectin-based formulations, although biodegradable, exhibited higher moisture sensitivity and faster initial drug release. In vitro release studies demonstrated a biphasic release pattern in alginate–chitosan systems, characterized by an initial burst followed by sustained release, predominantly governed by diffusion and polymer relaxation mechanisms. These findings highlight the potential of natural biopolymer matrices for improving the physicochemical stability and controlled release of amoxicillin, providing a sustainable alternative to conventional synthetic excipients. The study underscores the dual benefits of enhanced therapeutic performance and environmental sustainability, aligning with contemporary UK pharmaceutical priorities. Future work should explore in vivo pharmacokinetics and clinical translation to validate the therapeutic advantages of these formulations.
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M. A. Salam, M. Y. Al-Amin, M. T. Salam, J. S. Pawar, N. Akhter, A. A. Rabaan, dan M. A. A. Alqumber, “Antimicrobial Resistance: A Growing Serious Threat for Global Public Health,” Healthcare (Basel), vol. 11, no. 13, p. 1946, Jul. 2023.
M. R. Mithuna, R. Tharanyalakshmi, I. Jain, S. Singhal, D. Sikarwar, S. Das, J. Ranjitha, D. Ghosh, M. M. Rahman, dan B. Das, “Emergence of antibiotic resistance due to the excessive use of antibiotics in medicines and feed additives: A global scenario with emphasis on the Indian perspective,” Emerging Contaminants, vol. 10, no. 4, p. 100389, Dec. 2024.
A. N. F. Marzaman, T. P. Roska, S. Sartini, R. N. Utami, S. Sulistiawati, C. K. Enggi, M. A. Manggau, L. Rahman, V. P. Shastri, dan A. D. Permana, “Recent Advances in Pharmaceutical Approaches of Antimicrobial Agents for Selective Delivery in Various Administration Routes,” Antibiotics, vol. 12, no. 5, art. no. 822, 2023.
C. J. Parramon-Teixido, L. Rodríguez-Pombo, A. W. Basit, et al., “A framework for conducting clinical trials involving 3D printing of medicines at the point-of-care,” Drug Delivery and Translational Research, vol. 15, pp. 3078–3097, 2025.
E. Elhassan, C. A. Omolo, M. A. Gafar, et al., “Multifunctional hyaluronic acid-based biomimetic/pH-responsive hybrid nanostructured lipid carriers for treating bacterial sepsis,” Journal of Biomedical Science, vol. 32, art. no. 19, 2025.
B. Van Rooyen, M. De Wit, dan J. Van Niekerk, “Pectin and Alginate Functional Biopolymers: Factors Influencing Structural Composition, Functional Characteristics and Biofilm Development,” Coatings, vol. 14, no. 8, art. no. 987, 2024.
O. L. Orhotohwo, P. Lucci, A. K. Jaiswal, S. Jaiswal, dan D. Pacetti, “Enhancing the functional properties of chitosan-alginate edible films using spent coffee ground extract for fresh-cut fruit preservation,” Current Research in Food Science, vol. 11, p. 101124, Jun. 2025.
D. Thambavita, P. Galappatthy, U. Mannapperuma, L. Jayakody, R. Cristofoletti, B. Abrahamsson, D. W. Groot, P. Langguth, M. Mehta, A. Parr, J. E. Polli, V. P. Shah, dan J. Dressman, “Biowaiver Monograph for Immediate‑Release Solid Oral Dosage Forms: Amoxicillin Trihydrate,” Journal of Pharmaceutical Sciences, vol. 106, no. 10, pp. 2930‑2945, Oct. 2017.
B. J. Akhavan, N. R. Khanna, dan P. Vijhani, “Amoxicillin,” in StatPearls, Treasure Island, FL: StatPearls Publishing, 2025.
O. A. Omoteso, A. O. Fadaka, R. B. Walker, dan S. M. Khamanga, “Innovative Strategies for Combating Multidrug‑Resistant Tuberculosis: Advances in Drug Delivery Systems and Treatment,” Microorganisms, vol. 13, no. 4, art. no. 722, 2025.
R. Stancheva, T. Damyanova, T. Paunova‑Krasteva, R. Veleva, T. Topouzova‑Hristova, V. Ivanova, A. Trendafilova, I. Dimitrov, S. Rangelov, dan E. Haladjova, “Cationic Polymer Micelles as Carriers of Bioactive Sesquiterpene Lactones from Inula helenium L. for Effective Treatment of Bacterial Biofilms,” Pharmaceutics, vol. 17, no. 6, art. no. 800, 2025.
C. Bade, A. Olsacher, P. Boehme, H. Truebel, L. Bürger, dan L. Fehring, “Sustainability in the pharmaceutical industry an assessment of sustainability maturity and effects of sustainability measure implementation on supply chain security,” Corporate Social Responsibility and Environmental Management, vol. 31, no. 1, pp. 224‑242, Jan. 2024.
M. De Rosa, A. Verdino, A. Soriente, dan A. Marabotti, “The Odd Couple(s): An Overview of Beta‑Lactam Antibiotics Bearing More Than One Pharmacophoric Group,” International Journal of Molecular Sciences, vol. 22, no. 2, art. no. 617, Jan. 2021,
X. Lin dan U. Kück, “Cephalosporins as key lead generation beta-lactam antibiotics,” Applied Microbiology and Biotechnology, vol. 106, pp. 8007–8020, 2022.
K. Kamalpersad, G. Luna, B. Sunderland, dan P. Czarniak, “An Evaluation of Amoxicillin/Clavulanate Stability in Aqueous Systems, Including Its Suitability for Outpatient Parenteral Antimicrobial Therapy (OPAT),” Drug Design, Development and Therapy, vol. 18, pp. 4291–4301, Sep. 2024.
L. H. Ng, J. K. U. Ling, dan K. Hadinoto, “Formulation Strategies to Improve the Stability and Handling of Oral Solid Dosage Forms of Highly Hygroscopic Pharmaceuticals and Nutraceuticals,” Pharmaceutics, vol. 14, no. 10, art. no. 2015, Sep. 2022.
T. H. Tsung, Y. C. Tsai, H. P. Lee, Y. H. Chen, dan D. W. Lu, “Biodegradable Polymer-Based Drug-Delivery Systems for Ocular Diseases,” International Journal of Molecular Sciences, vol. 24, no. 16, art. no. 12976, Aug. 2023.
T. Aziz, A. Ullah, A. Ali, M. Shabeer, M. N. Shah, F. Haq, M. Iqbal, R. Ullah, dan F. U. Khan, “Manufactures of bio‑degradable and bio‑based polymers for bio‑materials in the pharmaceutical field,” Journal of Applied Polymer Science, vol. 139, no. 29, art. no. e52624, 2022.
M. Österberg, K. A. Henn, M. Farooq, dan J. J. Valle‑Delgado, “Biobased Nanomaterials─The Role of Interfacial Interactions for Advanced Materials,” Chemical Reviews, vol. 123, no. 5, pp. 2200‑2241, Mar. 2023.
F. G. Corrêa, R. J. P. Araujo, V. N. S. Campos, M. d. S. C. Silva, E. S. M. Cutrim, A. Rojas, M. M. Teixeira, M. A. S. Garcia, dan A. C. S. Alcântara, “Layered Double Hydroxides Modified with Carbon Quantum Dots as Promising Materials for Pharmaceutical Removal,” Minerals, vol. 15, no. 9, art. no. 899, 2025.
L. Salvioni, L. Morelli, E. Ochoa, M. Labra, L. Fiandra, L. Palugan, D. Prosperi, dan M. Colombo, “The emerging role of nanotechnology in skincare,” Advances in Colloid and Interface Science, vol. 293, p. 102437, Jul. 2021.
B. N. Estevinho, “Encapsulation Processes: Valorization, Stabilization, and Commercialization of Active and Natural Compounds,” Foods, vol. 14, no. 5, art. no. 844, Feb. 2025.
N. H. Thang, T. B. Chien, dan D. X. Cuong, “Polymer-Based Hydrogels Applied in Drug Delivery: An Overview,” Gels, vol. 9, no. 7, art. no. 523, Jun. 2023.
A. Geraili, M. Xing, dan K. Mequanint, “Design and fabrication of drug‑delivery systems toward adjustable release profiles for personalized treatment,” VIEW, vol. 2, no. 5, art. no. 20200126, May 2021.
D. U. Kapoor, R. Garg, M. Gaur, A. Pareek, B. G. Prajapati, G. R. Castro, S. Suttiruengwong, dan P. Sriamornsak, “Pectin hydrogels for controlled drug release: Recent developments and future prospects,” Saudi Pharmaceutical Journal, vol. 32, no. 4, art. no. 102002, Apr. 2024,
K. Bodnár, P. Fehér, Z. Ujhelyi, Á. Haimhoffer, B. Papp, D. Sinka, C. Freytag, E. Fidrus, K. Szarka, G. Kardos, F. Nacsa, I. Bácskay, dan L. Józsa, “Formulation and Testing of Alginate Microbeads Containing Salvia officinalis Extract and Prebiotics,” Pharmaceutics, vol. 17, no. 10, art. no. 1308, 2025.
M. Milivojević, A. Popović, I. Pajić‑Lijaković, I. Šoštarić, S. Kolašinac, dan Z. D. Stevanović, “Alginate Gel-Based Carriers for Encapsulation of Carotenoids: On Challenges and Applications,” Gels, vol. 9, no. 8, art. no. 620, Aug. 2023.
N. Jäck, S. Nagel, dan L. Hartmann, “Sequence‑defined polymers for biomedical applications,” Progress in Polymer Science, vol. 167, art. no. 101993, Aug. 2025.
B. G. Laycock, C. M. Chan, dan P. J. Halley, “A review of computational approaches used in the modelling, design, and manufacturing of biodegradable and biobased polymers,” Progress in Polymer Science, vol. 157, art. no. 101874, Oct. 2024.
A. Rezagholizade‑Shirvan, M. Soltani, S. Shokri, R. Radfar, M. Arab, dan E. Shamloo, “Bioactive compound encapsulation: Characteristics, applications in food systems, and implications for human health,” Food Chemistry: X, vol. 24, art. no. 101953, Dec. 2024.
C. D’Alessandro, K. Szopik‑Depczyńska, M. Tarczyńska‑Łuniewska, C. Silvestri, dan G. Ioppolo, “Exploring Circular Economy Practices in the Healthcare Sector: A Systematic Review and Bibliometric Analysis,” Sustainability, vol. 16, no. 1, art. no. 401, 2024.
K. Saha, Z. Farhanj, dan V. Kumar, “A Systematic Review of Circular Economy Literature in Healthcare: Transitioning from a ‘Post-Waste’ Approach to Sustainability,” Journal of Cleaner Production, 2025.
M. O’Dwyer, R. Filieri, dan L. O’Malley, “Establishing successful university–industry collaborations: barriers and enablers deconstructed,” Journal of Technology Transfer, vol. 48, pp. 900–931, 2023.
T. O. Machado, J. Grabow, C. Sayer, P. H. H. de Araújo, M. L. Ehrenhard, dan F. R. Wurm, “Biopolymer-based nanocarriers for sustained release of agrochemicals: A review on materials and social science perspectives for a sustainable future of agri- and horticulture,” Advances in Colloid and Interface Science, vol. 303, art. no. 102645, May 2022.
M. Dobrzyńska‑Mizera, J. M. Dodda, X. Liu, M. Knitter, R. N. Oosterbeek, P. Salinas, E. Pozo, A. M. Ferreira, et al., “Engineering of Bioresorbable Polymers for Tissue Engineering and Drug Delivery Applications,” Advanced Healthcare Materials, vol. 13, no. 30, art. no. 2401674, Sep. 2024.
