Evaluation of Ionotropic Cross-Linked Chitosan/Gelatin B Microspheres of Tramadol Hydrochloride
Open accessAbstract
Microspheres of tramadol hydrochloride (TM) for oral delivery were prepared by complex coacervation method without the use of chemical cross-linking agents such as glutaraldehyde to avoid the toxic reactions and other undesirable effects of the chemical cross-linking agents. Alternatively, ionotropic gelation was employed by using sodium-tripolyphosphate as cross-linking agent. Chitosan and gelatin B were used as polymer and copolymer, respectively. All the prepared microspheres were subjected to various physicochemical studies, such as drug-polymer compatibility by thin layer chromatography (TLC) and Fourier transform infrared (FTIR) spectroscopy, surface morphology by scanning electron microscopy, frequency distribution, drug entrapment efficiency, in vitro drug release characteristics and release kinetics. The physical state of drug in the microspheres was determined by differential scanning calorimetry (DSC) and X-ray diffractometry (XRD). TLC and FTIR studies indicated no drug-polymer incompatibility. All the microspheres showed initial burst release followed by a fickian diffusion mechanism. DSC and XRD analysis indicated that the TM trapped in the microspheres existed in an amorphous or disordered-crystalline status in the polymer matrix. From the preliminary trials, it was observed that it may be possible to formulate TM microspheres by using biodegradable natural polymers such as chitosan and gelatin B to overcome the drawbacks of TM and to increase the patient compliance.
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Amorphization may be attributed to polymer-drug interactions and microsphere fabrication conditions known to suppress drug crystallinity.
“This amorphization may be attributed to polymer-drug interactions and the conditions applied during microsphere fabrication, which are known to suppress drug crystallinity in polymer-based delivery systems.53”
From A bioinspired, pH-responsive microsphere matrix of cold-water extracted <i>Colocasia esculenta</i> mucilage and alginate: a new approach for sustained oral delivery of tramadol (2026) · cites this paper as [53]
The X-Ray Diffractometry section reports that tramadol was amorphous inside the microspheres and suggests preparation conditions as the cause. However, the Compatibility Studies section says FTIR ruled out drug–polymer interaction during preparation, so the proposed interaction is not supported. (LLM, conf=0.90)
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- Authors
- Basu, S. K., Kavitha, K., & Rupeshkumar, M.
- Affiliations
- Jadavpur University (IN)
- Corresponding author
- Kavitha, Kunchu
- ORCID
- Kavitha, Kunchu
- Venue
- AAPS PharmSciTech
- Published
- 2010-12-15
- Volume
- 12
- Issue
- 1
- Pages
- 28-34
- ISSN
- 1530-9932 (ISSN-L)
- PMC
- PMC3066349
- OpenAlex
- W2052996443
- Semantic Scholar
- 0edb592aa81b0165b3b48a2407b12a0456b3f7f8
- Cited by
- 29
- References
- 28
- Citations by year
- 2026: 3 · 2025: 1 · 2024: 2 · 2022: 3 · 2021: 4 · 2018: 1 · 2017: 2 · 2016: 4 · 2015: 2 · 2014: 4 · 2013: 2 · 2012: 1
- FWCI
- 0.67
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Licence
- www.springer.com/tdm (tdm)
- Locations
- AAPS PharmSciTech (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Indian Institute of Science
- Sun Pharma
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Medicine › Hydrogels: synthesis, properties, applications
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Keywords
- tramadol hydrochloride, ionic gelation, sodium tripolyphosphate, complex coacervation, oral drug delivery, drug-polymer compatibility, encapsulation efficiency, in vitro drug release kinetics, Fickian diffusion, amorphous drug state, burst release
- MeSH terms
- Analgesics, Opioid, Calorimetry, Differential Scanning, Cross-Linking Reagents, Diffusion, Drug Carriers, Gelatin, Humans, Microscopy, Electron, Scanning, Microspheres, Polyphosphates, Tramadol, Spectroscopy, Fourier Transform Infrared, Chitosan, In Vitro Techniques
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