Efavirenz nanomicelles loaded vaginal film (EZ film) for preexposure prophylaxis (PrEP) of HIV

Patki, Manali; Vartak, Richa; Jablonski, Joseph; Mediouni, Sonia; Gandhi, Tasneem; Fu, Yige; Cetindag, Eylul; Davé, Rajesh N.; Valente, Susana T.; Patel, Ketan

doi:10.1016/j.colsurfb.2020.111174

Cited by 17 publications

(11 citation statements)

References 45 publications

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“…The DSC thermograms of EZ bulk powder, PVA, FD-NS, and related physical mixture (PM) are depicted in Figure 4. A characteristic endotherm appeared for EZ at the onset temperature of 138.6°C, corresponding to the melting point of crystalline drug (39). The Thermogram of PVA revealed an endothermic peak in the range of 53.8 -65.3°C, related to its glass transition temperature.…”

Section: Dsc Ftir and Xrd Analysesmentioning

confidence: 96%

The Impact of Process and Formulation Parameters on the Fabrication of Efavirenz Nanosuspension to Improve Drug Solubility and Dissolution

2022

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Background: Efavirenz nanosuspensions (EZ-NSs) were developed by the wet milling method as the most promising top-down nanosizing technique. Different process and formulation parameters were studied and optimized to produce appropriate EZ-NS in suitable conditions to enhance drug dissolution. Methods: In the preliminary studies, various polymeric stabilizers, including Pluronic F68, sodium carboxymethylcellulose (CMC), hydroxypropyl methylcellulose (HPMC), and polyvinyl alcohol (PVA), as well as different sizes and weight of milling beads were used to prepare NSs. The effect of sodium lauryl sulfate (SLS) concentration on the NS properties was also evaluated. The influence of other formulation and process parameters, including polymer concentration, milling speed, and milling time, on the particle size and distribution of NSs were investigated using Box-Behnken design. The optimized freeze-dried nanosuspension was characterized by redispersibility, physicochemical properties, and stability. Results: A combination of PVA and SLS was selected as steric and electrostatic stabilizers. The optimum EZ-NS displayed a uniform size distribution with mean particle size and zeta potential of 254.4 nm and 21.1 mV, respectively. The solidified nanosuspension was well redispersed to the original nanoparticles. Significantly enhanced aqueous solubility (about 11-fold) and accelerated dissolution rate were observed for the optimized formulation. This could be attributed to the reduced particle size and partial amorphization of EZ during the preparation process, studied by X-ray diffraction. Accelerated studies confirmed the stability of the optimum freeze-dried formulation over the examined period of three months. Conclusions: Optimization of different variables led to the formation of EZ-NSs with desired properties through wet milling in a very short time compared to the previous study and therefore reduced production costs. This formulation seems to be a suitable approach for solubility and dissolution enhancement of EZ and may have great potential to improve the drug's oral bioavailability.

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Section: Dsc Ftir and Xrd Analysesmentioning

confidence: 96%

The Impact of Process and Formulation Parameters on the Fabrication of Efavirenz Nanosuspension to Improve Drug Solubility and Dissolution

2022

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“…Although vaginal films do not require an applicator to use, their possible influence during sexual intercourse is a disadvantage (Antimisiaris & Mourtas, 2015; Garg et al, 2010; Rohan et al, 2014). However, their formulation as a vaginal microbicide has been studied (Notario‐Perez et al, 2019; Notario‐Perez et al, 2020; Patki et al, 2020). Despite the microbicide formulation's progress, and most vaginal drugs have been in the form of gels, vaginal rings have gained acceptance in the last years due to a controlled release for a long time (Bunge et al, 2020; Katz et al, 2020; Roberts et al, 2020; Thurman et al, 2019; Vincent et al, 2018).…”

Section: Vaginal Formulations: Development and Characterizationmentioning

confidence: 99%

Baseline and time‐updated factors in preclinical development of anionic dendrimers as successful anti‐HIV‐1 vaginal microbicides

Rodriguez-Izquierdo

Sepúlveda‐Crespo

Lasso³

et al. 2022

WIREs Nanomed Nanobiotechnol

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Although a wide variety of topical microbicides provide promising in vitro and in vivo efficacy, most of them failed to prevent sexual transmission of human immunodeficiency virus type 1 (HIV-1) in human clinical trials. In vitro, ex vivo, and in vivo models must be optimized, considering the knowledge acquired from unsuccessful and successful clinical trials to improve the current gaps and the preclinical development protocols. To date, dendrimers are the only nanotool that has advanced to human clinical trials as topical microbicides to prevent HIV-1 transmission. This fact demonstrates the importance and the potential of these molecules as microbicides. Polyanionic dendrimers

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“…Both these issues can be overcome by formulating the molecules in surface-modified nanoparticles. Based on the physiological environment of the vagina and the obstacles that can interfere with nanoparticles, various modifications have also been explored [ 96 , 100 , 101 ].…”

Section: Vaginal Nanoformulations To Block Premature Cervix Remodelin...mentioning

confidence: 99%

Vaginal Nanoformulations for the Management of Preterm Birth

et al. 2022

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Preterm birth (PTB) is a leading cause of infant morbidity and mortality in the world. In 2020, 1 in 10 infants were born prematurely in the United States. The World Health Organization estimates that a total of 15 million infants are born prematurely every year. Current therapeutic interventions for PTB have had limited replicable success. Recent advancements in the field of nanomedicine have made it possible to utilize the vaginal administration route to effectively and locally deliver drugs to the female reproductive tract. Additionally, studies using murine models have provided important insights about the cervix as a gatekeeper for pregnancy and parturition. With these recent developments, the field of reproductive biology is on the cusp of a paradigm shift in the context of treating PTB. The present review focuses on the complexities associated with treating the condition and novel therapeutics that have produced promising results in preclinical studies.

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Efavirenz nanomicelles loaded vaginal film (EZ film) for preexposure prophylaxis (PrEP) of HIV

Cited by 17 publications

References 45 publications

The Impact of Process and Formulation Parameters on the Fabrication of Efavirenz Nanosuspension to Improve Drug Solubility and Dissolution

The Impact of Process and Formulation Parameters on the Fabrication of Efavirenz Nanosuspension to Improve Drug Solubility and Dissolution

Baseline and time‐updated factors in preclinical development of anionic dendrimers as successful anti‐HIV‐1 vaginal microbicides

Vaginal Nanoformulations for the Management of Preterm Birth

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