Amphiphilic triblock copolymers, based on hydrophilic poly(ethylene glycol) (PEG) blocks and hydrophobic poly(l,l-lactide) (PLLA) blocks, were used as the matrix material for the preparation of tetracycline-loaded microspheres. The morphology and thermal properties of the biodegradable microspheres were evaluated. SEM showed the predominance of the spherical shape, however, it was possible to distinguish three patterns: rough or smooth surface or uneven collapsed volume. The FTIR analysis indicated good mechanical stability and structural integrity of the PLLA-PEG-PLLA copolymer’s microspheres enclosing tetracycline. By thermal analysis it was possible to see the marginal influence of tetracycline on the glass transition and melting temperatures of the PLLA-PEG-PLLA triblock copolymer, while the results by TG indicated the presence of tetracycline in the inner structure of the microspheres, which thermal decomposition leading to char formation was triggered by the drug’s presence.
1. Sudhakar, Y, Kuotsu, K, Bandyopadhyay, AK. Buccal bioadhesive drug delivery–a promising option for orally less efficient drugs. J Control Rel. 2006;114:15–40. .
2. George, M, Abraham, TE. Polyionic hydrocolloids for the intestinal delivery of protein drugs: alginate and chitosan–a review. J Control Rel. 2006;114:1–15. .
3. Sajeesh, S, Sharma, CP. Cyclodextrin-insulin complex encapsulated polymethacrylic acid based nanoparticles for oral insulin delivery. Int J Pharm. 2006;325:17–29. .
4. Gupta, KC, Ravi Kumar, MNV. Drug release behavior of deads and microgranules of chitosan. Biomaterials. 2000;21:1115–1130. .
5. Liu, L, Li, C, Li, X, Yuan, Z, An, Y, He, B. Biodegradable polylactide/poly(ethylene glycol)/polylactide triblock copolymer micelles as anticancer drug carriers. J Appl Polym Sci. 2001;80:1976–1982. .
6. Deng, C, Rong, G, Tian, H, Tang, Z, Chen, X, Jing, X. Synthesis and characterization of poly(ethylene glycol)-b-poly(l-lactide)-b-poly(l-glutamic acid) triblock copolymer. Polymer. 2005;46:653–663. .
7. Kumar, N, Ravikumar, M, Domb, A. Biodegradable block copolymers. Adv Drug Deliv Rev. 2001;53:23–44. .
8. Mothé, CG, Drumond, WS, Wang, SH. Phase behavior of biodegradable amphiphilic poly(l, l-lactide)-b-poly(ethylene glycol)-b-poly(l, l-lactide). Thermochim Acta. 2006;445:61–66. .
9. Domingues, ZR, Cortés, ME, Gomes, TA, Diniz, HF, Freitas, CS, Gomes, JB, Faria, AMC, Sinisterra, RD. Bioactive glass as a drug delivery system of tetracycline and tetracycline associated with β-cyclodextrin. Biomaterials. 2004;25:327–334. .
10. Abdellaoui, KS, Monti, A, Barr, J, Heller, J, Gurny, R. Optimization of a novel bioerodible device based on auto-catalyzed poly(ortho esters) for controlled delivery of tetracycline to periodontal pocket. Biomaterials. 2001;22:1–14.
11. Drumond, WS, Mothé, CG, Wang, SH. Síntese e caracterização do copolímero poli (ácido lático-b-glicol etilenico). Polímeros Ciência Tecnol. 2004;14:74–79.
12. Bezemer, JM, Radersma, R, Grijpma, DW, Dijkstra, PJ, Van Blitterswijk, CA, Feijen, J. Microspheres for protein delivery prepared from amphiphilic multiblock copolymers 2. Modulation of release rate. J Control Rel. 2000;67:249–260. .
13. Yang, HJ, Park, IS, Na, K. Biocompatible microspheres based on acetylated polysaccharide prepared from water-in-oil-water (w1/o/w2) double-emulsion method for delivery of type II diabetic drug (exenatide). Colloid Surfaces Physicochem Eng Aspect. 2009;340:115–121. .
14. Choi, Y, Kim, SY, Kim, SH, Lee, KS, Kim, C, Byun, Y. Long-term delivery of all-trans-retinoic acid using biodegradable PLLA/PEG-PLLA blended microspheres. Int J Pharm. 2001;215:67–81. .
15. Souza, FB, Oliveira, MF, Lula, IS, Sansiviero, MTC, Cortés, ME, Sinisterra, RD. Study of inclusion compound in solution involving tetracycline and β-cyclodextrin by FTIR–ATR. Vib Spectrosc. 2008;46:57–66. .
16. Drumond, WS, Mothé, CG, Wang, SH. Quantitative analysis of biodegradable amphiphilic poly(l-lactide)block-poly(ethylene glycol)-block-poly(l-lactide) by using TG, FTIR and NMR. J Thermal Anal Calorim. 2006;85:173–177. .
17. Vila, A, Sánchez, A, Évora, C, Soriano, I, McCallion, O, Alonso, MJ. PLA-PEG particles as nasal protein carriers: the influence of the particle size. Int J Pharm. 2005;292:43–52. .
18. Yang, YY, Chung, TS, Ng, NP. Morphology, drug distribution and in vitro release profiles of biodegradable polymeric microspheres containing protein fabricated by double-emulsion solvent extraction/evaporation method. Biomaterials. 2001;22:231–241. .
19. Capan, Y, Jiang, G, Giovagnoli, S, Na, KH, DeLuca, PP. Preparation and characterization of poly(d,l-lactide-co-glycolide) microspheres for controlled release of human growth hormone. AAPS Pharm Sci Tech. 2003;4:1–10. .
20. Puapermpoonsiri, U, Spencer, J, Van der Walle, CF. A freeze-dried formulation of bacteriophage encapsulated in biodegradable microspheres. Eur J Pharm Biopharm. 2009;72:26–33. .
21. Ruan, G, Feng, SS. Preparation and characterization of poly(lactic acid)-poly(ethylene glycol)-poly(lactic acid) (PLA-PEG-PLA) microspheres for controlled release of paclitaxel. Biomaterials. 2003;24:5037–5044. .
22. Mothé, CG, Azevedo, AD, Drumond, WS, Wang, SH. Thermal properties of amphiphilic biodegradable triblock copolymer of l,l-lactide and ethylene glycol. J Thermal Anal Calorim. 2010;101: /1 229–233. .
23. Sharma, RK, Chan, WG, Seeman, JI, Hajaligol, MR. Formation of low molecular weight heterocycles and polycyclic aromatic compounds (PACs) in the pyrolysis of α-amino acids. J Anal Appl Pyrol. 2003;66:97–121. .
24. Ellis, TS. Miscibility of blends of aliphatic main-chain polyesters. Macromolecules. 1995;28:1882–1886. .
25. Moreno-Cerezo, JM, Córdoba-Díaz, M, Córdoba-Díaz, D, Córdoba-Borrego, M. A stability study of tetracycline and tetracycline cyclodextrins in pharmaceutical formulations. J Pharm Biom Anal. 2001;26:417–426. .