Screening of Sacrificial Excipients for Arresting Devitrification of Itraconazole from Solid Dispersion
Journal Title: Turkish Journal of Pharmaceutical Sciences - Year 2019, Vol 16, Issue 2
Abstract
Objectives: The aim of the present investigation was to develop a solid dispersion of itraconazole (ITR) using sacrificial excipients like pregelatinized starch and spray-dried lactose alongside hydroxypropyl methylcellulose and Poloxamer 188, thereby arresting the conversion of the amorphous form of ITR to crystalline form, and to assess the dissolution stability of an amorphous form of the drug during short-term storage. Materials and Methods: ITR-loaded solid dispersions were prepared by kneading. Formulation optimization was achieved by using a 24 full factorial design on the basis of cumulative percent drug released at t30, t60, and t120 min. An artificial neural network (ANN) was also applied as a statistical tool for obtaining better predictive ability and the outcomes of the ANN were compared with that of Design-Expert software. Results: The spectral data revealed no drug–carrier interactions. The P-X-ray diffraction study of the optimized batch showed a decrease in the crystallinity of drug as compared to the untreated drug. The in vitro dissolution studies of the optimized batch showed higher dissolution (92% at 120 min) in comparison to the other formulations. The dissolution stability study was performed at 40°C and 75% relative humidity for 90 days for the optimized formulation. The results of the optimized batch showed insignificant changes in cumulative percentage drug release during storage. Conclusion: Dissolution stability could be attributed to the presence of sacrificial excipients as they tend to absorb moisture during storage and possibly get converted into crystalline form, thereby minimizing the recrystallization of ITR.
Authors and Affiliations
Bhargavi M. PATEL, Mukesh C. GOHEL, Vaishali T. THAKKAR, Lalji H. BALDANIYA, Ruby R. CHRISTIAN, Tejal R. GANDHI
Investigation of Gelatinase Gene Expression and Growth of Enterococcus faecalis Clinical Isolates in Biofilm Models
Objectives: Enterococcus faecalis is the major reason for biofilm-related infections and it also interacts with Staphylococcus aureus in biofilms. Gelatinase (gelE) enzyme is an important virulence factor of E. faecalis...
Evaluation of the Possible Role of miRNAs in Chemical Allergen Potency
Objectives: MicroRNAs (miRNAs) are short, endogenous noncoding RNA molecules that can bind to certain parts of target mRNAs, thereby regulating gene expression. Studies showed that miRNAs could be up- or downregulated in...
Nanocarriers Used Most in Drug Delivery and Drug Release: Nanohydrogel, Chitosan, Graphene, and Solid Lipid
Over the past few years, nanocarriers have become an ideal solution for safe and efficient drug delivery and release. This is mainly due to the extraordinary characteristics that nanomaterials exhibit when compared with...
The Anticancer and Anti-inflammatory Effects of Centaurea solstitialis Extract on Human Cancer Cell Lines
Objectives: Natural products originating from plants have been used for many years in the treatment of various diseases, including cancer. Centaurea solstitialis subsp. solstitialis is used in Turkish folk medicine. This...
Fabrication and Evaluation of Transdermal Microneedles for a Recombinant Human Keratinocyte Growth Factor
Objectives: Microneedle transdermal patches are a combination of hypodermic needles and transdermal patches used to overcome the individual limitations of both injections and patches. The objective of this study was to d...