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Effect of lipid and cellulose based matrix former on the release of highly soluble drug from extruded/spheronized, sintered and compacted pellets.
Lipids Health Dis. 2018 Jun 09; 17(1):136.LH

Abstract

BACKGROUND

The study was to develop an extended release (ER) encapsulated and compacted pellets of Atenolol using hydrophobic (wax based and polymeric based) and high viscosity grade hydrophilic matrix formers to control the release of this highly water soluble drug by extrusion/spheronization (ES). Atenolol is used for cardiovascular diseases and available as an immediate release (IR) tablet dosage form. The lipids, Carnauba wax (CW), Glyceryl monostearate (GMS) and cellulose based i.e. Hydroxypropyl methylcellulose (HPMC) and Ethyl cellulose (EC) were used in preparing Atenolol ER pellets. Thermal sintering and compaction techniques were also applied to control the burst release of Atenolol.

METHOD

For this purpose, thirty-six trial formulations (F1-F36) were designed by Response Surface Methodology (RSM), using Design-Expert 10 software, keeping (HPMC K4M, K15 M & K100 M), (EC 7FP, 10FP & 100FP), waxes (GMS, & CW), their combinations, sintering temperature and duration, as input variables. Dissolution studies were performed in pH, 1.2, 4.5 and 6.8 dissolution media. Drug release kinetics using different models such as zero order, first order, Korsmeyer-Peppas, Hixon Crowell, Baker-Lonsdale and Higuchi kinetics were studied with the help of DDsolver, an excel based add-in program.

RESULTS

The formulations F35 and F36 showed compliance with Korsmeyer-Peppas Super case II transport model (R2 = 0.975-0.971) in dissolution medium pH 4.5. No drug excipient interaction observed by FTIR. Stereomicroscopy showed that sintered combination pellets, (F35), were highly spherical (AR = 1.061, and sphericity = 0.943). The cross-sectional SEM magnification (at 7000X) of F34 and F35 showed dense cross-linking. The results revealed that the optimized formulations were F35 (sintered pellets) and F36 (compacted pellets) effectively controlling the drug release for 12 h.

CONCLUSION

Extended-release encapsulated, and compacted pellets were successfully prepared after the combination of lipids CW (10%) and GMS (20%) with EC (10FP 20% & 100FP 20%). Sintering and compaction, in addition, stabilized the system and controlled the initial burst release of the drug. Extended release (ER) Atenolol is an effective alternative of IR tablets in controlling hypertension and treating other cardiovascular diseases.

Authors+Show Affiliations

Department of Pharmaceutics, Faculty of Pharmacy and Pharmaceutical Sciences, University of Karachi, Karachi, 75270, Pakistan. Faculty of Pharmacy, Jinnah University for Women, Karachi, 74600, Pakistan.Department of Pharmaceutics, Faculty of Pharmacy and Pharmaceutical Sciences, University of Karachi, Karachi, 75270, Pakistan.Department of Pharmaceutics, Faculty of Pharmacy and Pharmaceutical Sciences, University of Karachi, Karachi, 75270, Pakistan. harrisshoaib2000@yahoo.com.Department of Pharmaceutics, Faculty of Pharmacy and Pharmaceutical Sciences, University of Karachi, Karachi, 75270, Pakistan.Department of Pharmaceutics, Faculty of Pharmacy and Pharmaceutical Sciences, University of Karachi, Karachi, 75270, Pakistan.Department of Pharmaceutics, Faculty of Pharmacy and Pharmaceutical Sciences, University of Karachi, Karachi, 75270, Pakistan. Faculty of Pharmacy, Jinnah University for Women, Karachi, 74600, Pakistan.Department of Pharmaceutics, Faculty of Pharmacy and Pharmaceutical Sciences, University of Karachi, Karachi, 75270, Pakistan.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

29885655

Citation

Maboos, Madiha, et al. "Effect of Lipid and Cellulose Based Matrix Former On the Release of Highly Soluble Drug From Extruded/spheronized, Sintered and Compacted Pellets." Lipids in Health and Disease, vol. 17, no. 1, 2018, p. 136.
Maboos M, Yousuf RI, Shoaib MH, et al. Effect of lipid and cellulose based matrix former on the release of highly soluble drug from extruded/spheronized, sintered and compacted pellets. Lipids Health Dis. 2018;17(1):136.
Maboos, M., Yousuf, R. I., Shoaib, M. H., Nasiri, I., Hussain, T., Ahmed, H. F., & Iffat, W. (2018). Effect of lipid and cellulose based matrix former on the release of highly soluble drug from extruded/spheronized, sintered and compacted pellets. Lipids in Health and Disease, 17(1), 136. https://doi.org/10.1186/s12944-018-0783-8
Maboos M, et al. Effect of Lipid and Cellulose Based Matrix Former On the Release of Highly Soluble Drug From Extruded/spheronized, Sintered and Compacted Pellets. Lipids Health Dis. 2018 Jun 9;17(1):136. PubMed PMID: 29885655.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effect of lipid and cellulose based matrix former on the release of highly soluble drug from extruded/spheronized, sintered and compacted pellets. AU - Maboos,Madiha, AU - Yousuf,Rabia Ismail, AU - Shoaib,Muhammad Harris, AU - Nasiri,Iqbal, AU - Hussain,Tazeen, AU - Ahmed,Hafiza Fouzia, AU - Iffat,Wajiha, Y1 - 2018/06/09/ PY - 2018/04/30/received PY - 2018/05/16/accepted PY - 2018/6/11/entrez PY - 2018/6/11/pubmed PY - 2018/10/31/medline KW - Atenolol KW - Carnauba wax (CW) KW - Ethyl cellulose (EC) KW - Extended release KW - Extrusion-Spheronization KW - Fourier transform spectroscopy (FTIR) KW - Glyceryl monostearate (GMS) KW - Hydroxypropyl methylcellulose (HPMC) KW - Pellets KW - Scanning Electron microscopy (SEM) SP - 136 EP - 136 JF - Lipids in health and disease JO - Lipids Health Dis VL - 17 IS - 1 N2 - BACKGROUND: The study was to develop an extended release (ER) encapsulated and compacted pellets of Atenolol using hydrophobic (wax based and polymeric based) and high viscosity grade hydrophilic matrix formers to control the release of this highly water soluble drug by extrusion/spheronization (ES). Atenolol is used for cardiovascular diseases and available as an immediate release (IR) tablet dosage form. The lipids, Carnauba wax (CW), Glyceryl monostearate (GMS) and cellulose based i.e. Hydroxypropyl methylcellulose (HPMC) and Ethyl cellulose (EC) were used in preparing Atenolol ER pellets. Thermal sintering and compaction techniques were also applied to control the burst release of Atenolol. METHOD: For this purpose, thirty-six trial formulations (F1-F36) were designed by Response Surface Methodology (RSM), using Design-Expert 10 software, keeping (HPMC K4M, K15 M & K100 M), (EC 7FP, 10FP & 100FP), waxes (GMS, & CW), their combinations, sintering temperature and duration, as input variables. Dissolution studies were performed in pH, 1.2, 4.5 and 6.8 dissolution media. Drug release kinetics using different models such as zero order, first order, Korsmeyer-Peppas, Hixon Crowell, Baker-Lonsdale and Higuchi kinetics were studied with the help of DDsolver, an excel based add-in program. RESULTS: The formulations F35 and F36 showed compliance with Korsmeyer-Peppas Super case II transport model (R2 = 0.975-0.971) in dissolution medium pH 4.5. No drug excipient interaction observed by FTIR. Stereomicroscopy showed that sintered combination pellets, (F35), were highly spherical (AR = 1.061, and sphericity = 0.943). The cross-sectional SEM magnification (at 7000X) of F34 and F35 showed dense cross-linking. The results revealed that the optimized formulations were F35 (sintered pellets) and F36 (compacted pellets) effectively controlling the drug release for 12 h. CONCLUSION: Extended-release encapsulated, and compacted pellets were successfully prepared after the combination of lipids CW (10%) and GMS (20%) with EC (10FP 20% & 100FP 20%). Sintering and compaction, in addition, stabilized the system and controlled the initial burst release of the drug. Extended release (ER) Atenolol is an effective alternative of IR tablets in controlling hypertension and treating other cardiovascular diseases. SN - 1476-511X UR - https://www.unboundmedicine.com/medline/citation/29885655/Effect_of_lipid_and_cellulose_based_matrix_former_on_the_release_of_highly_soluble_drug_from_extruded/spheronized_sintered_and_compacted_pellets_ L2 - https://lipidworld.biomedcentral.com/articles/10.1186/s12944-018-0783-8 DB - PRIME DP - Unbound Medicine ER -