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The Impact of Lithocholic Acid as A Surfactant on the Characteristics and Cytocompatibility of Azithromycin Loaded Self-Emulsifying Drug Delivery System
EP37547
Poster Title: The Impact of Lithocholic Acid as A Surfactant on the Characteristics and Cytocompatibility of Azithromycin Loaded Self-Emulsifying Drug Delivery System
Submitted on 18 Aug 2021
Author(s): Reem Abou Assi1,2, Ibrahim M.Abdulbaqi1,2, Toh Seok Ming1, Chan Siok Yee1*, Habibah A. Wahab1*, Yusrida Darwis1*
Affiliations: 1 The Discipline of Pharmaceutical Technology, School of Pharmaceutical Sciences, Universiti Sains Malaysia, 11800, Penang, Malaysia. The Discipline of Pharmaceutical Technology, College of Pharmacy, Al-Kitab University, Altun kupri, Kirkuk, Iraq.
This poster was presented at Malaysian Pharmacist Society-National Pharmacists Convention 2021
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Poster Information
Abstract: Introduction: The self-emulsifying drug delivery system (SEDDS) has emerged as an effective pharmaceutical strategy for addressing the issue of poorly soluble drug bioavailability, specifically candidates belonging to BCS classes II and IV including azithromycin (AZM, log p = 4). Aside from oil, the main component in SEDDS is the surfactant, which is presented in high concentrations leading to complex physiological interactions raising the possibility of toxicity. Surfactants derived from bile acid have transpired as an excellent choice of bio-compatible pharmaceutical excipient. Unconjugated lithocholic acid (LA) has recently been reported to improve formulations’ drug release and stability. Objective: To investigate LA as a safe and effective surfactant in liquid SEDDS (L-SEDDS), and compare it with LA-free L-SEDDS and solid SEDDS (S-SEDDS) states of AZM. This is in terms of reduced particle size (PS), dispersity (Đ), self-emulsification efficiency (T%), zeta potential charge in distilled water (DW), 0.1 mM HCl, and simulated intestinal fluids (SIF), as well as cellular viability. Method: L-SEDDS was formulated with Capryol 90® oil (22.22%), Tween 20® as surfactant and Transcutol HP® (2:1 ratio) as co-surfactant. S-SEDDS was produced by adsorbing the L-SEDDS(s) to Aerosil 200® as a solid carrier (at 2:1 ratio of L-SEDDs to Aerosil 200®). In L-SEDDS, LA was incorporated at high (B-L-SEDDS3), medium (B-L-SEDDS2), and low (B-L-SEDDS1) concentrations of 7.75, 3.6, and 1.03 mg/ml respectively. Later, AZM was loaded. MTT assay was performed on human Colon carcinoma cell lines. Results and Discussion: Significant reduction in PS, and Đ values was observed upon the addition of LA (p<0.05) in both blank and loaded B-L-SEDDS and compared to LA-free AZM-loaded liquid and solid SEDDSs, respectively. Besides, the size reduction was LA concentration-dependent and could be advantageous for drug absorption and lymphatic uptake, while the Đ reduction represents SEDDS improved homogeneity. After the addition of LA, T% increased up to ~ 100%, while ZP charges were negative in DW and SIF, with charge shift to positive in HCl diluent. Almost all SEDDSs formulations exhibited good cytocompatibility (> ~85%). Conclusion: LA is a potential surfactant for desired features of SEDDS (PS, Đ and T%) with a good safety profile.Summary: feature of SEDDS with a good safety profile. This study revealed the significant role of using bile acids LA as surfactants in SEDDS formulation for particle size reduction and enhanced homogeneity. The high transmittance reveals the successful formation of the colloid system upon emulsification. Furthermore, the developed system showed cytocompatibility which indicates its safety. Therefore, lithocholic acid is a potential surfactant for desired
References: 1. Pavlović, N. et al., Bile Acids and Their Derivatives as Potential Modifiers of Drug Release and Pharmacokinetic Profiles, Front. Pharmacol., 2018, 9,1283.
2. Wagle, S.R. et al., Pharmacological and Advanced Cell Respiration Effects, Enhanced by Toxic Human-Bile Nano-Pharmaceuticals of Probucol Cell-Targeting Formulations. Pharmaceutics 2020,12,708
3. Mathavan, S., et. al.,. A comprehensive study of novel microcapsules incorporating gliclazide and a permeation enhancing bile acid: Hypoglycemic effect in an animal model of Type-1 diabetes. Drug Deliv. 2016, 23, 2869–2880
4. Abou Assi, R.et. al., Liquid and Solid Self-Emulsifying Drug Delivery Systems (SEDDs) as Carriers for the Oral Delivery of Azithromycin: Optimization, In Vitro Characterization and Stability Assessment, Pharmaceutics 2020,12,1052.
5. Choi, et al., Positively Charged Nanostructured Lipid Carriers and Their Effect on the Dissolution of Poorly Soluble Drugs, Molecules. 2016;21(5):672.
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