Formulation and development of thermosensitive cyclodextrin-based in situ gel of voriconazole for vaginal delivery

Deshkar, Sanjeevani Shekhar; Palve, Vidyanand Kundlik

doi:10.1016/j.jddst.2018.11.023

Cited by 46 publications

(28 citation statements)

References 34 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Carbon dioxide gas was used with a flow rate of 120 L/min. The system's level of residual oxygen was regulated below 4% [8,43].…”

Section: Spray Drying Methods (Sd)mentioning

confidence: 99%

Host-guest inclusion complex of desloratadine with 2-(hydroxy)propyl-?-cyclodextrin (HP-?-CD): Preparation, binding behaviors and dissolution properties

Kırımlıoğlu¹

2020

jrp

View full text Add to dashboard Cite

Desloratadine (DSL) is an anti-allergic agent that diminishes nasal and non-nasal allergic marks of seasonal allergic rhinitis. However, its efficiency of DSL is restricted with its low dissolution rate and aqueous solubility. The influence of 2-(hydroxy)propyl-β-cyclodextrin (HP-β-CD) on the DSL solubility was evaluated in respect of the phase solubility method. Following the formulation of inclusion complexes of DSL and HP-β-CD with various strategies (freeze-drying, spray-drying and kneading) (FD, SD and KN), compounds were investigated to evaluate the possibility of altering the physicochemical properties (solubility, release, stability, morphology) of DSL after complexation that are critical for subsequent formulation studies including the complexes prepared. Changes in DSC thermograms, FT-IR spectra and NMR spectra confirmed the constitution of a DSL-HP-β-CD complexes. In vitro release from inclusion complexes was compared to pure DSL by dialysis method. It was found that solubility enhancements of DSL-HP-β-CD complexes relies on the sort of the formulation technique. Higher release of DSL from complexes compared to pure DSL was ascribed to the interactive relations between HP-β-CD and DSL, high energetic amorphous status and inclusion complex constitution.

show abstract

“…Carbon dioxide gas was used with a flow rate of 120 L/min. The system's level of residual oxygen was regulated below 4% [8,43].…”

Section: Spray Drying Methods (Sd)mentioning

confidence: 99%

Host-guest inclusion complex of desloratadine with 2-(hydroxy)propyl-?-cyclodextrin (HP-?-CD): Preparation, binding behaviors and dissolution properties

Kırımlıoğlu¹

2020

jrp

View full text Add to dashboard Cite

show abstract

“…To study the effect of dilution on the gelling temperature of in situ gelling formulations, citrate buffer pH 4.8 was added (0.25 ml per g of gel) to 4 g of formulations in a vial. The gelling temperature of the diluted formulation was determined using a previously described method (Deshkar and Palve, 2019;Cai, 2011).…”

Section: Effect Of Dilution On Gelling Temperaturementioning

confidence: 99%

“…The formulations were graded as, No Phase transition (-), the formation of the gel after 60 S and collapsed rapidly within 15min (+), the formation of the gel after 60 S and gel collapsed within1 h (++), the formation of gel within 60 S and did not collapse till six h. (+++). Each sample was measured in triplicate (Deshkar and Palve, 2019).…”

Section: Gelling Abilitymentioning

confidence: 99%

“…The absorbance of the iltrate was measured at 254.0 nm by UV spectro photometer using methanol and distilled water mixture as blank. The per cent drug content of the gel formulation was calculated using a calibration curve of ACV in the same solvent (Deshkar and Palve, 2019).…”

Section: Drug Contentmentioning

confidence: 99%

“…The force required to detach the gels from goat vaginal tissue was measured asmucoadhesive strength (g). The readings were taken in triplicate on the same vaginal mucosa (Deshkar and Palve, 2019;Han et al, 2006).…”

Section: Mucoadhesion Strengthmentioning

confidence: 99%

See 2 more Smart Citations

Formulation and Evaluation of Microemulsion Based in Situ Gel of Acyclovir for Vaginal Delivery

Deshkar

Bokare

Todmal

2020

ijrps

View full text Add to dashboard Cite

The purpose of the present study was to formulate and evaluate microemulsion based in situ gel of Acyclovir (ACV) for the vaginal delivery. The solubility of ACV in oils and surfactants and co-surfactant was evaluated to identify the components of the microemulsion. Microemulsion region was determined by using the pseudo-ternary phase diagrams for different formulations. Microemulsion formulation was prepared using Labrafil M1994C as oil phase, Cremophor RH40 as surfactant and Polyethylene glycol 400 and Transcutol P as co-surfactant and water. Microemulsion formulations were evaluated for pH, viscosity, conductivity and stability study. In situ gel of ACV, microemulsion was prepared using thermosensitive polymer, poloxamer.In situ gelwas characterized for viscosity, gelling temperature, the effect of dilution on gelling temperature, gelling ability, and in vitro drug release and release kinetics. The globule size of developed microemulsion was less than 100 nm with PDI in the range 0.307 to 0.641. The optimized microemulsion based in situ gel demonstrated shear thinning behaviour, the gelation temperature with and without dilution was in the range of 30-35ºC, and the drug release was sustained over eight hours. Mucoadhesive properties of microemulsion based in situ gel formulations were determined with a texture analyzer using a goat vaginal tissue, and the results indicated that the presence of microemulsion increased the mucoadhesion significantly. Microemulsion based in situ gel was successfully developed for vaginal delivery of Acyclovir.

show abstract

Vaginal Bioadhesive Drug Delivery Systems and Their Applications

Deshkar

Shirolkar

Patil

2020

Bioadhesives in Drug Delivery

View full text Add to dashboard Cite

Formulation and development of thermosensitive cyclodextrin-based in situ gel of voriconazole for vaginal delivery

Cited by 46 publications

References 34 publications

Host-guest inclusion complex of desloratadine with 2-(hydroxy)propyl-?-cyclodextrin (HP-?-CD): Preparation, binding behaviors and dissolution properties

Host-guest inclusion complex of desloratadine with 2-(hydroxy)propyl-?-cyclodextrin (HP-?-CD): Preparation, binding behaviors and dissolution properties

Formulation and Evaluation of Microemulsion Based in Situ Gel of Acyclovir for Vaginal Delivery

Vaginal Bioadhesive Drug Delivery Systems and Their Applications

Contact Info

Product

Resources

About