Promethazine-montmorillonite inclusion complex to enhance drug photostability

Valeria Ambrogi1, Morena Nocchetti, Loredana Latterini

  • 1Dipartimento di Scienze Farmaceutiche and ‡Dipartimento di Chimica, Biologia e Biotecnologie, Università degli Studi di Perugia , 06123 Perugia, Italy.

Insights

Montmorillonite (MONT) effectively enhances the photostability of photolabile drugs like promethazine (PRO). Intercalating PRO into MONT significantly slows its degradation, offering improved drug photoprotection.

Area of Science:

  • Materials Science
  • Pharmaceutical Science
  • Photochemistry

Background:

  • Photolabile drugs are susceptible to degradation upon light exposure, limiting their therapeutic applications.
  • Montmorillonite (MONT) has emerged as a promising matrix for enhancing drug photostability.
  • Understanding drug-matrix interactions is crucial for developing stable pharmaceutical formulations.

Purpose of the Study:

  • To investigate the photoprotective effects of montmorillonite (MONT) on promethazine (PRO), a model photolabile drug.
  • To characterize the intercalated hybrid material (MONT-PRO) and evaluate its photostability.
  • To assess the potential of MONT-PRO for pharmaceutical formulation.

Main Methods:

  • Drug intercalation of promethazine (PRO) into montmorillonite (MONT).
  • Characterization using X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), and FTIR spectroscopy.
  • Photostability evaluation through spectrophotometric measurements and nanosecond transient absorption spectroscopy.

Main Results:

  • Successful preparation of MONT-PRO hybrid material with high drug loading.
  • Markedly improved photostability of PRO intercalated in MONT, with a 5-fold slower degradation rate compared to homogeneous solutions.
  • Suppression of drug photoionization and reduced singlet oxygen production due to matrix interaction.

Conclusions:

  • Montmorillonite (MONT) significantly enhances the photostability of promethazine (PRO).
  • The MONT-PRO intercalation compound demonstrates improved photoprotection, making it suitable for pharmaceutical applications.
  • MONT-PRO can be formulated into gels or ointments without compromising photostability.

Related Concept Videos

Bioavailability Enhancement: Drug Stability Enhancement and GI Retention01:05

Bioavailability Enhancement: Drug Stability Enhancement and GI Retention

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...
320
Bioavailability Enhancement: Drug Solubility Enhancement01:16

Bioavailability Enhancement: Drug Solubility Enhancement

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...
470
Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence01:27

Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence

Changes in polymorphic forms can significantly influence the bioavailability of poorly soluble drugs. Although the FDA defines pharmaceutical equivalence based on having the same active ingredient, dosage form, and route of administration, it does not automatically disqualify products with different polymorphic forms. This means two products with different polymorphs can still be deemed pharmaceutically equivalent. However, polymorphic differences can affect properties like wettability,...
227
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,...
327
Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism01:21

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism

Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
897