Formulation and characterization of self-nanoemulsifying drug delivery systems containing monoacyl phosphatidylcholine

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• 作者：Thuy Tran^a ; Xi Xi^a ; Thomas Rades^a ; Anette Mü ; llertz^a ; ^b ; ^{anette.mullertz@sund.ku.dk" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Cryo-TEM ; cryogenic transmission electron microscopy ; DoE ; design of experiments ; FaSSGFTDC ; fasted-state simulated gastric fluid containing sodium taurodeoxycholate ; FaMIF ; fasted-state median intestinal fluid ; LC ; long-chain ; LPC ; Lipoid S LPC 80 ; MAPC ; monoacyl phosphatidylcholine ; MC ; medium-chain ; PC ; phosphatidylcholine ; SNEDDS ; self-nanoemulsifying drug delivery systems
• 刊名：International Journal of Pharmaceutics
• 出版年：2016
• 出版时间：11 April 2016
• 年：2016
• 卷：502
• 期：1-2
• 页码：151-160
• 全文大小：1918 K

文摘

The study investigated the use of monoacyl phosphatidylcholine (MAPC) in self-nanoemulsifying drug delivery system (SNEDDS). A D-optimal design was used to generate two sets of formulations containing long-chain (LC) or medium-chain (MC) glycerides, caprylocaproyl macrogol-8 glycerides (Labrasol), Lipoid S LPC 80 (LPC) (80% MAPC) and ethanol. The formulations were characterized using dynamic light scattering, microscopy, in vitro lipolysis and viscometric measurements. All LC formulations within the investigated range were predicted to generate polydisperse emulsions while MC formulations generated nanoemulsions with droplet sizes from 23 to 167 nm. Using LPC in MC formulations reduced the nanoemulsion droplet sizes in simulated gastric and intestinal media. The nanoemulsion droplet size of MC SNEDDS containing LPC was not affected by gastrointestinal pH, while the zeta potentials increased at low pH. During in vitro lipolysis, less fatty acids were released when LPC was incorporated into the formulations (2.05 ± 0.02 mmol reduced to 1.76 ± 0.05 mmol when incorporating 30% LPC). Replacing Labrasol by LPC increased the formulation dynamic viscosity from 57 ± 1 mPa s (0% LPC) to 436 ± 8 mPa s (35% LPC) at 25 °C, however, this did not considerably prolong the formulation dispersion time. In conclusion, MC SNEDDS containing LPC are promising formulations when desiring to reduce the amount of synthetic surfactants and possibly modify the digestion rate.