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Characterization and evaluation of solid self-microemulsifying drug delivery systems with porous carriers as systems for improved carbamazepine release.
Int J Pharm. 2012 Oct 15; 436(1-2):58-65.IJ

Abstract

The purpose of this study was to investigate solid self-microemulsifying drug delivery system (SSMEDDS), as potential delivery system for poorly water soluble drug carbamazepine (CBZ). Self-microemulsifying drug delivery system (SMEDDS) was formulated using the surfactant polyoxyethylene 20 sorbitan monooleate [Polysorbate 80] (S), the cosurfactant PEG-40 hydrogenated castor oil [Cremophor(®) RH40] (C) and the oil caprylic/capric triglycerides [Mygliol(®) 812] (O). Four different adsorbents with high specific surface area were used: Neusilin(®) UFL2, Neusilin(®) FL2 (magnesium aluminometasilicate), Sylysia(®) 320 and Sylysia(®) 350 (porous silica). Microemulsion area at the surfactant to cosurfactant ratio (K(m)) 1:1 was evaluated and for further investigation SMEDDS with SC/O ratio 8:2 was selected. Solubilization capacity of selected SMEDDS for CBZ was 33.771±0.041 mg/ml. Rheological measurements of unloaded and CBZ-loaded SMEDDS at water content varied from 10 to 60% (w/w) were conducted. It has been found that CBZ has great influence on rheological behaviour of investigated system upon water dilution. Photon correlation spectroscopy has shown the ability of CBZ-loaded SMEDDS to produce microemulsion droplet size. SSMEDDS improved release rate of CBZ, but the type of adsorbent significantly affects release rate of CBZ. For SSMEDDS with different magnesium aluminometasilicate adsorbents, release rate of CBZ decreased with increasing specific surface area due to entrapment of liquid SMEDDS inside the pores and its gradual exposure to dissolution medium. With porous silica adsorbents no difference in release rate was found in comparison to physical mixtures. In physical mixtures at 12.5% (w/w) CBZ content, presence of amorphous CBZ led to high dissolution rate.

Authors+Show Affiliations

Department of Pharmaceutical Technology and Cosmetology, University of Belgrade, Faculty of Pharmacy, Vojvode Stepe 450, P.O. Box 146, 11221 Belgrade, Serbia.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

22721847

Citation

Milović, Mladen, et al. "Characterization and Evaluation of Solid Self-microemulsifying Drug Delivery Systems With Porous Carriers as Systems for Improved Carbamazepine Release." International Journal of Pharmaceutics, vol. 436, no. 1-2, 2012, pp. 58-65.
Milović M, Djuriš J, Djekić L, et al. Characterization and evaluation of solid self-microemulsifying drug delivery systems with porous carriers as systems for improved carbamazepine release. Int J Pharm. 2012;436(1-2):58-65.
Milović, M., Djuriš, J., Djekić, L., Vasiljević, D., & Ibrić, S. (2012). Characterization and evaluation of solid self-microemulsifying drug delivery systems with porous carriers as systems for improved carbamazepine release. International Journal of Pharmaceutics, 436(1-2), 58-65. https://doi.org/10.1016/j.ijpharm.2012.06.032
Milović M, et al. Characterization and Evaluation of Solid Self-microemulsifying Drug Delivery Systems With Porous Carriers as Systems for Improved Carbamazepine Release. Int J Pharm. 2012 Oct 15;436(1-2):58-65. PubMed PMID: 22721847.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Characterization and evaluation of solid self-microemulsifying drug delivery systems with porous carriers as systems for improved carbamazepine release. AU - Milović,Mladen, AU - Djuriš,Jelena, AU - Djekić,Ljiljana, AU - Vasiljević,Dragana, AU - Ibrić,Svetlana, Y1 - 2012/06/18/ PY - 2012/03/30/received PY - 2012/05/31/revised PY - 2012/06/11/accepted PY - 2012/6/23/entrez PY - 2012/6/23/pubmed PY - 2013/1/17/medline SP - 58 EP - 65 JF - International journal of pharmaceutics JO - Int J Pharm VL - 436 IS - 1-2 N2 - The purpose of this study was to investigate solid self-microemulsifying drug delivery system (SSMEDDS), as potential delivery system for poorly water soluble drug carbamazepine (CBZ). Self-microemulsifying drug delivery system (SMEDDS) was formulated using the surfactant polyoxyethylene 20 sorbitan monooleate [Polysorbate 80] (S), the cosurfactant PEG-40 hydrogenated castor oil [Cremophor(®) RH40] (C) and the oil caprylic/capric triglycerides [Mygliol(®) 812] (O). Four different adsorbents with high specific surface area were used: Neusilin(®) UFL2, Neusilin(®) FL2 (magnesium aluminometasilicate), Sylysia(®) 320 and Sylysia(®) 350 (porous silica). Microemulsion area at the surfactant to cosurfactant ratio (K(m)) 1:1 was evaluated and for further investigation SMEDDS with SC/O ratio 8:2 was selected. Solubilization capacity of selected SMEDDS for CBZ was 33.771±0.041 mg/ml. Rheological measurements of unloaded and CBZ-loaded SMEDDS at water content varied from 10 to 60% (w/w) were conducted. It has been found that CBZ has great influence on rheological behaviour of investigated system upon water dilution. Photon correlation spectroscopy has shown the ability of CBZ-loaded SMEDDS to produce microemulsion droplet size. SSMEDDS improved release rate of CBZ, but the type of adsorbent significantly affects release rate of CBZ. For SSMEDDS with different magnesium aluminometasilicate adsorbents, release rate of CBZ decreased with increasing specific surface area due to entrapment of liquid SMEDDS inside the pores and its gradual exposure to dissolution medium. With porous silica adsorbents no difference in release rate was found in comparison to physical mixtures. In physical mixtures at 12.5% (w/w) CBZ content, presence of amorphous CBZ led to high dissolution rate. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/22721847/Characterization_and_evaluation_of_solid_self_microemulsifying_drug_delivery_systems_with_porous_carriers_as_systems_for_improved_carbamazepine_release_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(12)00630-8 DB - PRIME DP - Unbound Medicine ER -