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Bioavailability Enhancement: Drug Stability Enhancement and GI Retention01:05

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Body:Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
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Bioavailability Enhancement: Drug Solubility Enhancement01:16

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Body:Bioavailability is a critical factor in determining a drug's effectiveness. It refers to the proportion of a drug that enters the circulation when introduced into the body and is, as a result, able to have an active effect. Enhancing bioavailability is essential for drugs with poor solubility, as it can significantly impact their therapeutic efficacy. Various methods are employed to increase the solubility of drugs, thereby enhancing their bioavailability.Micronization and nanonization are...
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Bioavailability Enhancement: Drug Permeability Enhancement01:27

Bioavailability Enhancement: Drug Permeability Enhancement

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Body: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...
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A loading dose is an essential pharmacological strategy to rapidly achieve the target plasma drug concentration necessary for an immediate therapeutic effect. This approach is especially critical for drugs characterized by slow absorption or extended half-lives, where delaying therapeutic plasma levels could compromise treatment outcomes. By administering a loading dose, clinicians ensure a prompt onset of drug action, even for agents with complex pharmacokinetic profiles.Achieving steady-state...
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Bioavailability: Influencing Factors01:22

Bioavailability: Influencing Factors

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Bioavailability refers to the extent and rate at which a drug reaches systemic circulation in its active form. Extent refers to the amount of the drug that makes it into circulation, while rate is the speed at which it enters circulation. It is influenced by several factors critical for optimizing drug formulations, dosing regimens, and therapeutic outcomes.Physicochemical properties of drugs and formulationsThe solubility, stability, and dissolution rate of a drug significantly impact its...
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Morin hydrate loaded solid lipid nanoparticles: Characterization, stability, anticancer activity, and

Swathi Karamchedu1, Lakshmi Tunki2, Hitesh Kulhari3

  • 1Department of Bioanalytical Sciences, Ramnarain Ruia College, Mumbai, 400019, India.

Chemistry and Physics of Lipids
|October 9, 2020
PubMed
Summary

This study developed morin hydrate loaded solid lipid nanoparticles (MSN) to improve anticancer drug delivery. Encapsulated morin hydrate showed enhanced cytotoxicity and pharmacokinetics against cervical cancer cells.

Keywords:
Anticancer activityBioavailabilityMorin hydrateSolid lipid nanoparticlesStability

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Area of Science:

  • Nanotechnology
  • Drug Delivery Systems
  • Bioflavonoids

Background:

  • Morin hydrate (MH) is a natural anticancer bioflavonoid with poor aqueous solubility and low oral bioavailability.
  • Solid lipid nanoparticles (SLNs) offer a promising nanocarrier system for improving drug delivery.
  • Encapsulating hydrophobic drugs into SLNs can enhance their therapeutic efficacy.

Purpose of the Study:

  • To encapsulate morin hydrate (MH) into solid lipid nanoparticles (MSN).
  • To overcome the poor aqueous solubility and low oral bioavailability of MH.
  • To evaluate the in vitro anticancer activity and pharmacokinetic profile of MSN.

Main Methods:

  • Preparation and characterization of morin hydrate loaded solid lipid nanoparticles (MSN) using DLS, FTIR, and DSC.
  • In vitro release studies in simulated intestinal fluid.
  • In vitro anticancer studies against human cervical cancer cells.
  • Pharmacokinetic evaluation of encapsulated MH.

Main Results:

  • MSN exhibited nanoscale size and good steric stability.
  • MSN demonstrated controlled release of MH in simulated intestinal fluid.
  • Encapsulated MH in MSN showed significantly higher cytotoxicity against cervical cancer cells compared to free MH.
  • MSN significantly improved the pharmacokinetic properties of encapsulated MH.

Conclusions:

  • Solid lipid nanoparticles are effective nanocarriers for morin hydrate delivery.
  • MSN enhance the anticancer efficacy of morin hydrate against cervical cancer.
  • This nanomedicine approach holds potential for improved cancer therapy.