Formulation Development of Albendazole-Loaded Self-Microemulsifying Chewable Tablets to Enhance Dissolution and Bioavailability

Albendazole is an anthelmintic agent with poor solubility and absorption. We developed a chewable tablet (200 mg drug equivalent), containing a self-microemulsifying drug delivery system (SMEDDS), with oral disintegrating properties. The emulsion was developed using sesame and soybean oils along wit...

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Main Authors: Somchai Sawatdee, Apichart Atipairin, Attawadee Sae Yoon, Teerapol Srichana, Narumon Changsan, Tan Suwandecha
Format: Article
Language:English
Published: MDPI AG 2019-03-01
Series:Pharmaceutics
Subjects:
Online Access:https://www.mdpi.com/1999-4923/11/3/134
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author Somchai Sawatdee
Apichart Atipairin
Attawadee Sae Yoon
Teerapol Srichana
Narumon Changsan
Tan Suwandecha
author_facet Somchai Sawatdee
Apichart Atipairin
Attawadee Sae Yoon
Teerapol Srichana
Narumon Changsan
Tan Suwandecha
author_sort Somchai Sawatdee
collection DOAJ
description Albendazole is an anthelmintic agent with poor solubility and absorption. We developed a chewable tablet (200 mg drug equivalent), containing a self-microemulsifying drug delivery system (SMEDDS), with oral disintegrating properties. The emulsion was developed using sesame and soybean oils along with surfactant/co-surfactants, and the tablets were prepared by wet granulation using superdisintegrants and adsorbents. Infra-red (IR) spectral studies revealed no interaction between the drug and excipients, and all physical and chemical parameters were within acceptable limits. Stability studies for the formulation indicated no significant change over time. An in vitro release study indicated 100% drug release within 30 min, and in vivo plasma concentrations indicated that the area under the curve (AUC) of albendazole in rats administered SMEDDS chewable tablets was significantly higher than in those administered commercial tablets or powder (<i>p</i>-value &lt; 0.05). The systemic bioavailability of albendazole achieved through the SMEDDS tablets was 1.3 times higher than that achieved by the administration of comparable quantities of albendazole commercial tablets. This was due to the higher dissolution of albendazole SMEDDS in the chewable tablets. We conclude that the SMEDDS chewable formulation can be used to improve the dissolution and systemic availability of poorly water-soluble drugs.
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spelling doaj.art-373bbfa9707d42f98bc41997a3d273ec2022-12-22T04:20:10ZengMDPI AGPharmaceutics1999-49232019-03-0111313410.3390/pharmaceutics11030134pharmaceutics11030134Formulation Development of Albendazole-Loaded Self-Microemulsifying Chewable Tablets to Enhance Dissolution and BioavailabilitySomchai Sawatdee0Apichart Atipairin1Attawadee Sae Yoon2Teerapol Srichana3Narumon Changsan4Tan Suwandecha5Drug and Cosmetics Excellence Center, Walailak University, Thasala, Nakhon Si Thammarat 80161, ThailandDrug and Cosmetics Excellence Center, Walailak University, Thasala, Nakhon Si Thammarat 80161, ThailandDrug and Cosmetics Excellence Center, Walailak University, Thasala, Nakhon Si Thammarat 80161, ThailandDrug Delivery System Excellence Center and Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Songkhla 90112, ThailandFaculty of Pharmacy, Rangsit University, Pathumtani 12000, ThailandDepartment of Pharmacology, Faculty of Sciences, Prince of Songkla University, Hat Yai, Songkhla 90112, ThailandAlbendazole is an anthelmintic agent with poor solubility and absorption. We developed a chewable tablet (200 mg drug equivalent), containing a self-microemulsifying drug delivery system (SMEDDS), with oral disintegrating properties. The emulsion was developed using sesame and soybean oils along with surfactant/co-surfactants, and the tablets were prepared by wet granulation using superdisintegrants and adsorbents. Infra-red (IR) spectral studies revealed no interaction between the drug and excipients, and all physical and chemical parameters were within acceptable limits. Stability studies for the formulation indicated no significant change over time. An in vitro release study indicated 100% drug release within 30 min, and in vivo plasma concentrations indicated that the area under the curve (AUC) of albendazole in rats administered SMEDDS chewable tablets was significantly higher than in those administered commercial tablets or powder (<i>p</i>-value &lt; 0.05). The systemic bioavailability of albendazole achieved through the SMEDDS tablets was 1.3 times higher than that achieved by the administration of comparable quantities of albendazole commercial tablets. This was due to the higher dissolution of albendazole SMEDDS in the chewable tablets. We conclude that the SMEDDS chewable formulation can be used to improve the dissolution and systemic availability of poorly water-soluble drugs.https://www.mdpi.com/1999-4923/11/3/134albendazoleself-microemulsionchewable tabletdissolutionbioavailabilitypharmacokinetics
spellingShingle Somchai Sawatdee
Apichart Atipairin
Attawadee Sae Yoon
Teerapol Srichana
Narumon Changsan
Tan Suwandecha
Formulation Development of Albendazole-Loaded Self-Microemulsifying Chewable Tablets to Enhance Dissolution and Bioavailability
Pharmaceutics
albendazole
self-microemulsion
chewable tablet
dissolution
bioavailability
pharmacokinetics
title Formulation Development of Albendazole-Loaded Self-Microemulsifying Chewable Tablets to Enhance Dissolution and Bioavailability
title_full Formulation Development of Albendazole-Loaded Self-Microemulsifying Chewable Tablets to Enhance Dissolution and Bioavailability
title_fullStr Formulation Development of Albendazole-Loaded Self-Microemulsifying Chewable Tablets to Enhance Dissolution and Bioavailability
title_full_unstemmed Formulation Development of Albendazole-Loaded Self-Microemulsifying Chewable Tablets to Enhance Dissolution and Bioavailability
title_short Formulation Development of Albendazole-Loaded Self-Microemulsifying Chewable Tablets to Enhance Dissolution and Bioavailability
title_sort formulation development of albendazole loaded self microemulsifying chewable tablets to enhance dissolution and bioavailability
topic albendazole
self-microemulsion
chewable tablet
dissolution
bioavailability
pharmacokinetics
url https://www.mdpi.com/1999-4923/11/3/134
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AT attawadeesaeyoon formulationdevelopmentofalbendazoleloadedselfmicroemulsifyingchewabletabletstoenhancedissolutionandbioavailability
AT teerapolsrichana formulationdevelopmentofalbendazoleloadedselfmicroemulsifyingchewabletabletstoenhancedissolutionandbioavailability
AT narumonchangsan formulationdevelopmentofalbendazoleloadedselfmicroemulsifyingchewabletabletstoenhancedissolutionandbioavailability
AT tansuwandecha formulationdevelopmentofalbendazoleloadedselfmicroemulsifyingchewabletabletstoenhancedissolutionandbioavailability