Execution of Quality by Design Approach in the Formulation of Fluconazole Inclusion Complex Based Suppository for Vaginal Candidiasis

ABSTRACT

Aim: The present work was carried out to improve the aqueous solubility of Fluconazole by formulation of inclusion complex using β-cyclodextrin and then loaded into the suppository for the treatment of vaginal candidiasis. Material and Methods: Fluconazole (FOZ) Inclusion Complex (INC) with β-Cyclodextrin (βCD) was formulated first after optimization of the D-Optimal mixture design for the molar ratio. Then INC was prepared (1:1 molar ratio) with different methods (kneading, coprecipitation and microwave irradiation) and was studied for FTIR, DSC and XRD studies. Results: Microwave irradiation (MW) was the best method for the preparation of INC with the maximum % drug content (98.96±1.78%) and solubility (3.14±0.85 mg/mL). The QbD approach was employed to select the best ratio of the base and plasticizer for the suppository. The suppository was prepared using PEG 6000 (base) and PEG 400 (plasticizer) and an optimized inclusion complex was incorporated. The D-Optimal mixture design was applied to optimize a combination of PEG 6000 and PEG 400 by studying responses such as hardness, melting time and drug release from the suppository. The in vitro release study showed that higher drug release was achieved from the FOZ MW INC based suppository (99.40±1.43%) compared to the plain drug suppository (71.41±2.19%). Conclusion: The prepared FOZ suppository had higher drug release and enhanced antifungal activity. Therefore, it would be beneficial in the treatment of Vaginal Candidiasis.

KEYWORDS

• D-Optimal mixture design
• Fluconazole
• Inclusion complex
• Solubility enhancement
• Vaginal Candidiasis
• β-cyclodextrin

Showing references and in-text citations exactly as published.

• DOI10.5530/ijper.20256191Copy

RELATED ARTICLES

Matched on section and article type within this issue of IJPER.

• Article · VOLUME 59, ISSUE 2SA Qualitative Study on Lecture Capturing System in Pharmacy Education-Learners’ PerspectiveSaranraj Loganathan, Rajkumaran Soundarraj, Vishwalingam Murugan Sujetha · pp. s410–s413Original ArticleSame type: Article
• Article · VOLUME 59, ISSUE 2SFormulation and Evaluation of Simvastatin Loaded Nanostructured Lipid Carrier for Topical Drug DeliveryMadhuri Desai, Shalaka Dhanna, Sujata Jadhav, Akshada Koparde, Akansha Dashwanat, Rutuja Gharal · pp. s414–s425Original ArticleSame type: Article
• Article · VOLUME 59, ISSUE 2SOptimized Vildagliptin Microsphere Formulation and in vitro Characterization Using 23 Factorial Design AnalysisSundaramoorthi Revathi, Pavadai Anitha, Sathappan Jenifer, Sivakumar Senthil Rajan · pp. s426–s435Original ArticleSame type: Article
• Article · VOLUME 59, ISSUE 2SBilosome Nanocarriers for Enhanced Oral Bioavailability and Cardiovascular Activity of MilrinoneKiruthika Santhinathan, Susmitha Durai, Rijivana Sirajudeen, Gopinath Govindhraji, Saravanan Gopal, Gayathri Kumararaja · pp. s436–s442Original ArticleSame type: Article