Development and evaluation of calcium alginate beads prepared by sequential and simultaneous methods
The objective of this study was to develop a sustained release dosage form of Trimetazidine dihydrochloride (TMZ) using a natural polymeric carrier prepared in a completely aqueous environment. TMZ was entrapped in calcium alginate beads prepared with sodium alginate by the ionotropic gelation metho...
| Main Authors: | , , , |
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| Format: | Article |
| Language: | English |
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Universidade de São Paulo
2010-12-01
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| Series: | Brazilian Journal of Pharmaceutical Sciences |
| Subjects: | |
| Online Access: | http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502010000400021 |
| _version_ | 1818755041384726528 |
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| author | Sanchita Mandal S. Senthil Kumar Balakrishnam Krishnamoorthy Sanat Kumar Basu |
| author_facet | Sanchita Mandal S. Senthil Kumar Balakrishnam Krishnamoorthy Sanat Kumar Basu |
| author_sort | Sanchita Mandal |
| collection | DOAJ |
| description | The objective of this study was to develop a sustained release dosage form of Trimetazidine dihydrochloride (TMZ) using a natural polymeric carrier prepared in a completely aqueous environment. TMZ was entrapped in calcium alginate beads prepared with sodium alginate by the ionotropic gelation method using calcium chloride as a crosslinking agent. The drug was incorporated either into preformed calcium alginate gel beads (sequential method) or incorporated simultaneously during the gelation stage (simultaneous method). The beads were evaluated for particle size and surface morphology using optical microscopy and SEM, respectively. Beads produced by the sequential method had higher drug entrapment. Drug entrapment in the sequential method was higher with increased CaCl2 and polymer concentration but lower with increased drug concentration. In the simultaneous method, drug entrapment was higher when polymer and drug concentration were increased and also rose to a certain extent with increase in CaCl2 concentration, where further increase resulted in lower drug loading. FTIR studies revealed that there is no interaction between drug and CaCl2. XRD studies showed that the crystalline drug changed to an amorphous state after formulation. Release characteristics of the TMZ loaded calcium alginate beads were studied in enzyme-free simulated gastric and intestinal fluid.<br>O objetivo deste estudo foi desenvolver forma de liberação controlada de dicloridrato de trimetazidina (TMZ) utilizando transportador plomérico natural em ambiente completamente aquoso. A TMZ foi presa em pérolas de alginato de cálcio preparadas com alginato de sódio pelo método de gelatinização ionotrópica, usando cloreto de cálcio como agente de formação de ligações cruzadas. O fármaco foi incorporado nas pérolas de gel de alginato de cálcio (método sequencial) ou incorporado, simultaneamente, durante o estágio de gelificação (método simultâneo). As pérolas foram avaliadas quanto ao tamanho das partículas e morfologia da superfície utilizando microscopia óptica de SEM, respectivamente. As pérolas produzidas pelo método sequencial apresentaram maior capacidade de inclusão. No método sequencial, a inclusão de fármaco foi maior com o aumento de CaCl2 e da concentração do plímero, mas menor com o aumento da concentração de fármaco. No método simultâneo, a inclusão de fármaco foi mais alta quando as concentrações de fármaco e plímero foram aumentadas e, também, atingiram certa extensão com aumento na concentração de CaCl2, cujo aumento posterior resultou em carga menor de fármaco. Estudos de FTIR revelaram que não há interação entre fármaco e CaCl2. Estudos de XRD mostraram que o fármaco mudou do estado cristalino para o amorfo após a formulação. As características de liberação de TMZ das pérolas carregadas com alginato de cálcio foram estudadas em fluidos simulados, gástrico e intestinal, livres de enzima. |
| first_indexed | 2024-12-18T05:32:50Z |
| format | Article |
| id | doaj.art-f4bb81361d79451ba1a3a685f833d880 |
| institution | Directory Open Access Journal |
| issn | 1984-8250 2175-9790 |
| language | English |
| last_indexed | 2024-12-18T05:32:50Z |
| publishDate | 2010-12-01 |
| publisher | Universidade de São Paulo |
| record_format | Article |
| series | Brazilian Journal of Pharmaceutical Sciences |
| spelling | doaj.art-f4bb81361d79451ba1a3a685f833d8802022-12-21T21:19:24ZengUniversidade de São PauloBrazilian Journal of Pharmaceutical Sciences1984-82502175-97902010-12-0146478579310.1590/S1984-82502010000400021Development and evaluation of calcium alginate beads prepared by sequential and simultaneous methodsSanchita MandalS. Senthil KumarBalakrishnam KrishnamoorthySanat Kumar BasuThe objective of this study was to develop a sustained release dosage form of Trimetazidine dihydrochloride (TMZ) using a natural polymeric carrier prepared in a completely aqueous environment. TMZ was entrapped in calcium alginate beads prepared with sodium alginate by the ionotropic gelation method using calcium chloride as a crosslinking agent. The drug was incorporated either into preformed calcium alginate gel beads (sequential method) or incorporated simultaneously during the gelation stage (simultaneous method). The beads were evaluated for particle size and surface morphology using optical microscopy and SEM, respectively. Beads produced by the sequential method had higher drug entrapment. Drug entrapment in the sequential method was higher with increased CaCl2 and polymer concentration but lower with increased drug concentration. In the simultaneous method, drug entrapment was higher when polymer and drug concentration were increased and also rose to a certain extent with increase in CaCl2 concentration, where further increase resulted in lower drug loading. FTIR studies revealed that there is no interaction between drug and CaCl2. XRD studies showed that the crystalline drug changed to an amorphous state after formulation. Release characteristics of the TMZ loaded calcium alginate beads were studied in enzyme-free simulated gastric and intestinal fluid.<br>O objetivo deste estudo foi desenvolver forma de liberação controlada de dicloridrato de trimetazidina (TMZ) utilizando transportador plomérico natural em ambiente completamente aquoso. A TMZ foi presa em pérolas de alginato de cálcio preparadas com alginato de sódio pelo método de gelatinização ionotrópica, usando cloreto de cálcio como agente de formação de ligações cruzadas. O fármaco foi incorporado nas pérolas de gel de alginato de cálcio (método sequencial) ou incorporado, simultaneamente, durante o estágio de gelificação (método simultâneo). As pérolas foram avaliadas quanto ao tamanho das partículas e morfologia da superfície utilizando microscopia óptica de SEM, respectivamente. As pérolas produzidas pelo método sequencial apresentaram maior capacidade de inclusão. No método sequencial, a inclusão de fármaco foi maior com o aumento de CaCl2 e da concentração do plímero, mas menor com o aumento da concentração de fármaco. No método simultâneo, a inclusão de fármaco foi mais alta quando as concentrações de fármaco e plímero foram aumentadas e, também, atingiram certa extensão com aumento na concentração de CaCl2, cujo aumento posterior resultou em carga menor de fármaco. Estudos de FTIR revelaram que não há interação entre fármaco e CaCl2. Estudos de XRD mostraram que o fármaco mudou do estado cristalino para o amorfo após a formulação. As características de liberação de TMZ das pérolas carregadas com alginato de cálcio foram estudadas em fluidos simulados, gástrico e intestinal, livres de enzima.http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502010000400021Alginato de sódioBeads de alginato de cálcioDicloridrato de trimetazidinaGelatinização ionotrópicaSodium alginateCalcium alginate beadsTrimetazidine dihydrochlorideIonotropic gelation |
| spellingShingle | Sanchita Mandal S. Senthil Kumar Balakrishnam Krishnamoorthy Sanat Kumar Basu Development and evaluation of calcium alginate beads prepared by sequential and simultaneous methods Brazilian Journal of Pharmaceutical Sciences Alginato de sódio Beads de alginato de cálcio Dicloridrato de trimetazidina Gelatinização ionotrópica Sodium alginate Calcium alginate beads Trimetazidine dihydrochloride Ionotropic gelation |
| title | Development and evaluation of calcium alginate beads prepared by sequential and simultaneous methods |
| title_full | Development and evaluation of calcium alginate beads prepared by sequential and simultaneous methods |
| title_fullStr | Development and evaluation of calcium alginate beads prepared by sequential and simultaneous methods |
| title_full_unstemmed | Development and evaluation of calcium alginate beads prepared by sequential and simultaneous methods |
| title_short | Development and evaluation of calcium alginate beads prepared by sequential and simultaneous methods |
| title_sort | development and evaluation of calcium alginate beads prepared by sequential and simultaneous methods |
| topic | Alginato de sódio Beads de alginato de cálcio Dicloridrato de trimetazidina Gelatinização ionotrópica Sodium alginate Calcium alginate beads Trimetazidine dihydrochloride Ionotropic gelation |
| url | http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502010000400021 |
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