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Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
Preparation and characterization of a biodegradable drug targeting system for anticancer drug delivery:
Asli Muvaffak1, Ismet Gurhan, Ufuk Gunduz
1Department of Surgery, Harvard Medical School, Beth Israel Deaconess Medical Center, Boston, MA 02215, USA. amuvaffa@bidmc.harvard.edu
Abstract:
Targeted delivery of anticancer drugs is one of the most actively pursued goals in anticancer chemotherapy. A major disadvantage of anticancer drugs is their lack of selectivity for tumour tissue, which causes severe side effects and results in low cure rates. Any strategy by which a cytotoxic drug is targeted to the tumour, thus increasing the therapeutic index of the drug, is a way of improving cancer chemotherapy and minimizing systematic toxicity. This study covers the preparation of the gelatin microsphere (GM)-anti-bovine serum albumin (anti-BSA) conjugate for the development of a drug targeting approach for anticancer drug delivery. Microspheres of 5% (w/v) gelatin content were prepared by crosslinking with glutaraldehyde (GTA) at 0.05 and 0.50% (v/v) concentration. Microspheres were in the size range of 71-141?microm. The suitability of these microspheres as drug carriers for anticancer drug delivery was investigated in vitro by studying the release profiles of loaded methotrexate (MTX) and 5-fluorouracil (5-FU) and the cytotoxicities on cancer cell lines. The in vitro MTX release profiles (approximately 22-46% released in 24 h depending on the amount of GTA used) were much slower compared to 5-FU (approximately 42-91% released in 24 h). Both drugs demonstrated an initial fast release, which was followed by gradual, sustained drug release. The MTT cytotoxicity test results of GMs loaded with 5-FU and MTX showed approximately 54-70% and approximately 52-67% cytotoxicities in 4 days. In general, incorporation of MTX and 5-FU in microspheres enhanced the cytotoxic effect in a more prolonged manner compared to the free drugs. Gelatin micospheres were chemically conjugated to anti-BSA and the antigen-antibody activities were studied by immunofluorescence. Results indicated approximately 80% binding with conjugated anti-BSA and BSA-FITC. Based on their low cytotoxicity and the high antigen binding efficiencies, anti-BSA conjugated gelatin microspheres could be suitable targeted drug carrier systems for selective and long-term delivery of anticancer drugs to a specific body compartment (i.e. bladder cancer).
Insights
Researchers developed gelatin microspheres (GM) conjugated with anti-bovine serum albumin (anti-BSA) for targeted anticancer drug delivery. These microspheres show potential for selective, long-term delivery of chemotherapy drugs like methotrexate and 5-fluorouracil, reducing side effects.
Area of Science:
- Biomaterials Science
- Nanotechnology in Medicine
- Oncology Drug Delivery
Background:
- Conventional chemotherapy suffers from poor tumor selectivity, leading to severe systemic toxicity and limited efficacy.
- Targeted drug delivery systems aim to enhance the therapeutic index of anticancer agents by concentrating them at the tumor site.
- Gelatin microspheres (GM) offer a biodegradable platform for drug encapsulation and controlled release applications.
Purpose of the Study:
- To prepare and characterize gelatin microspheres (GM) conjugated with anti-bovine serum albumin (anti-BSA) for targeted anticancer drug delivery.
- To evaluate the in vitro drug release kinetics of methotrexate (MTX) and 5-fluorouracil (5-FU) from GMs.
- To assess the in vitro cytotoxicity of drug-loaded GMs and the antigen-antibody binding efficiency of the conjugated microspheres.
Main Methods:
- Gelatin microspheres were prepared using glutaraldehyde (GTA) crosslinking at varying concentrations (0.05% and 0.50%).
- Microspheres were loaded with methotrexate (MTX) and 5-fluorouracil (5-FU), and their release profiles were studied in vitro.
- Cytotoxicity was evaluated using MTT assays on cancer cell lines, and antigen-antibody activity was confirmed by immunofluorescence.
Main Results:
- Gelatin microspheres (71-141 μm) were successfully prepared and conjugated with anti-BSA, showing approximately 80% binding efficiency.
- In vitro drug release showed sustained release profiles for both MTX (22-46% in 24h) and 5-FU (42-91% in 24h), influenced by GTA concentration.
- Drug-loaded GMs demonstrated enhanced and prolonged cytotoxic effects on cancer cell lines compared to free drugs.
Conclusions:
- Anti-BSA conjugated gelatin microspheres are promising carriers for targeted and sustained delivery of anticancer drugs.
- The system exhibits potential for selective delivery to specific tissues, such as in bladder cancer treatment.
- This approach could significantly improve chemotherapy by increasing drug efficacy and minimizing systemic toxicity.
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