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Bioavailability Enhancement: Drug Permeability Enhancement01:27

Bioavailability Enhancement: Drug Permeability Enhancement

After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt secretion,...
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Bioequivalence in generic drugs, such as tablets and capsules, refers to their pharmaceutical equivalence to the brand-name counterparts. However, for therapeutic equivalence, manufacturers must also consider physical attributes like size, shape, and weight (FDA Guidance for Industry, December 2003). Discrepancies in these aspects could impact patient compliance and cause medication errors. For instance, swallowing difficulties, often experienced with larger tablets or capsules, can lead to...

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Updated: Jun 18, 2026

Preparation and Characterization of Nanoliposomes for the Entrapment of Bioactive Hydrophilic Globular Proteins
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Published on: August 31, 2019

Formulation, Characterization, and Biological Assessment of Embelin-Loaded Glycerosomes.

Monika Dhaka1, Md Habban Akhter1, Maha Alsunbul2

  • 1Faculty of Pharmacy, DIT University, Dehradun, India.

Assay and Drug Development Technologies
|June 17, 2026
PubMed
Summary

Embelin-loaded glycerosomes (GLSMs) were developed to overcome low bioavailability issues. These novel GLSMs show enhanced liver drug delivery, improved oral bioavailability, and potent lipid-lowering and hepatoprotective effects for liver disease treatment.

Keywords:
Box–Behnken designembelinglycerosomesmetabolic dysfunction-associated steatotic liver diseasepharmacokinetics

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Area of Science:

  • Pharmaceutical Nanotechnology
  • Drug Delivery Systems
  • Medicinal Chemistry

Background:

  • Embelin (EB) possesses significant hepatoprotective properties but is limited by poor solubility and low oral bioavailability.
  • Existing therapeutic limitations necessitate advanced delivery systems to enhance embelin's clinical efficacy.
  • Glycerosomes (GLSMs) represent a promising vesicular nanocarrier for improving drug delivery and bioavailability.

Purpose of the Study:

  • To develop and characterize embelin-loaded glycerosomes (EB-GLSMs) for enhanced oral bioavailability and targeted liver delivery.
  • To optimize EB-GLSM formulation using a Box-Behnken design for improved physicochemical properties.
  • To evaluate the in vitro and in vivo performance of EB-GLSMs, including pharmacokinetic and therapeutic effects.

Main Methods:

  • EB-GLSMs were prepared via thin-film hydration and optimized using a 3^2 Box-Behnken design.
  • Formulations were characterized for vesicle size, polydispersity index, zeta potential, and entrapment efficiency.
  • In vitro drug release studies, transmission electron microscopy, and in vivo pharmacokinetic and lipid-lowering studies in rats were conducted.

Main Results:

  • Optimized EB-GLSMs showed a vesicle size of 214.41 nm, PDI of 0.145, zeta potential of -30 mV, and 94.74% entrapment efficiency.
  • Transmission electron microscopy confirmed uniform, spherical vesicles. Sustained drug release over 12 hours was observed.
  • In vivo studies demonstrated a 2.5-fold increase in plasma bioavailability, significant reduction in serum triglycerides and cholesterol, and enhanced hepatoprotective effects compared to aqueous embelin suspension.

Conclusions:

  • Developed EB-loaded glycerosomes significantly enhance embelin's oral bioavailability and liver drug delivery.
  • The optimized EB-GLSM formulation exhibits promising sustained-release properties and potent lipid-lowering and hepatoprotective activities.
  • EB-GLSMs represent a viable therapeutic strategy for managing liver diseases.