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- 저자 : Alagar Balakumar (검색결과 1 건)
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Lacidipine self-nanoemulsifying drug delivery system for the enhancement of oral bioavailability
Natesan Subramanian,Shanmugam Palaniappan Sharavanan,Ponnusamy Chandrasekar,Alagar Balakumar,Satya Priya Moulik 대한약학회 2016 Archives of Pharmacal Research Vol.39 No.4
Low bioavailability of Lacidipine (LD), ancalcium channel blocker pose many challenges in thetreatment of hypertension. The objective of this study wasto formulate and characterize LD self-nanoemulsifyingdrug delivery systems (SNEDDS) to improve oralbioavailability of the drug. Formulations were evaluatedfor globule size, surface morphology, emulsification time,cloud point, drug content, in vitro dissolution, ex vivopermeation, stability and oral bioavailability studies. Captex810D, TPGS, Tween-60, Transcutol P and PEG 400was selected based on the solubility study results. Theoptimized SNEDDS readily gets nanoemulsified at 37 Cwith droplet size of 41 nm when mixed with 200 times ofits water. Transmission electron microscope photographsconfirmed the spherical shape of the globules. In vitrodissolution of SNEDDS showed more than 80 % of drugrelease within 15 min. The ex vivo permeation of LD fromSNEDDS is 4.8- and 9-fold higher compared to pure drugin the absence and presence of verapamil respectively. Thestability study of the SNEDDS confirmed no environmentaleffect on the physical nature and drug content. Oralbioavailability of SNEDDS is 2.5 times higher than marketedtablet. The results suggest that, the SNEDDS formulationcan be used as a possible alternative for thetraditional oral formulations of LD to improve its oralbioavailability.
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