Oral self-emulsifying nanoemulsion systems for enhancing dissolution, bioavailability and anticancer effects of camptothecin

Galatage, Sunil T.; Trivedi, Rahul; Bhagwat, Durgacharan A.

doi:10.1016/j.jddst.2022.103929

Cited by 10 publications

(3 citation statements)

References 69 publications

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“…Furthermore, F1 exhibited the highest release percentage due to its low oil content and high S-mixture content. This composition results in a reduced requirement of free energy to create new interfaces between the lipid and water phases [ 76 ]. Moreover, DSC and FIIR confirmed the amorphous state of the drug in the NE and indicated the complete solubility of the drug in the NE base [ 77 ].…”

Section: Discussionmentioning

confidence: 99%

Aceclofenac/Citronellol Oil Nanoemulsion Repurposing Study: Formulation, In Vitro Characterization, and In Silico Evaluation of Their Antiproliferative and Pro-Apoptotic Activity against Melanoma Cell Line

Younis,

Khalil,

Younis

et al. 2023

Biomedicines

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Aceclofenac (ACF) is a widely used non-steroidal anti-inflammatory drug (NSAID) known for its effectiveness in treating pain and inflammation. Recent studies have demonstrated that ACF possesses antiproliferative properties, inhibiting the growth of cancer cells in various cancer cell lines. Citronellol, a monoterpenoid alcohol found in essential oils, exhibits antioxidant properties and activities such as inhibiting cell growth and acetylcholinesterase inhibition. In this study, the objective was to formulate and evaluate an aceclofenac/citronellol oil nanoemulsion for its antiproliferative effects on melanoma. The optimal concentrations of citronellol oil, Tween 80, and Transcutol HP were determined using a pseudoternary phase diagram. The formulated nanoemulsions were characterized for droplet size, zeta potential, thermophysical stability, and in vitro release. The selected formula (F1) consisted of citronellol oil (1 gm%), Tween 80 (4 gm%), and Transcutol HP (1 gm%). F1 exhibited a spherical appearance with high drug content, small droplet size, and acceptable negative zeta potential. The amorphous state of the drug in the nanoemulsion was confirmed by Differential Scanning Calorimetry, while FTIR analysis indicated its homogenous solubility. The nanoemulsion showed significant antiproliferative activity, with a lower IC50 value compared to aceclofenac or citronellol alone. Flow cytometric analysis revealed cell cycle arrest and increased apoptosis induced by the nanoemulsion. In silico studies provided insights into the molecular mechanism underlying the observed antitumor activity. In conclusion, the developed aceclofenac/citronellol oil nanoemulsion exhibited potent cytotoxicity and pro-apoptotic effects, suggesting its potential as a repurposed antiproliferative agent for melanoma treatment. In a future plan, further animal model research for validation is suggested.

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Section: Discussionmentioning

confidence: 99%

Aceclofenac/Citronellol Oil Nanoemulsion Repurposing Study: Formulation, In Vitro Characterization, and In Silico Evaluation of Their Antiproliferative and Pro-Apoptotic Activity against Melanoma Cell Line

Younis,

Khalil,

Younis

et al. 2023

Biomedicines

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“…The ternary phase diagrams (Figure 2) were constructed to determine the concentration range of components required to form a stable nano-emulsion. The darker region in the phase diagram represented the self-emulsification area [50]. It was observed that the addition of surfactant-cosurfactant improved the efficiency of emulsification due to their higher hydrophilicity properties [51].…”

Section: Construction Of Pseudo-ternary Phase Diagrammentioning

confidence: 99%

Development and Evaluation of a Self-Nanoemulsifying Drug Delivery System for Sinapic Acid with Improved Antiviral Efficacy against SARS-CoV-2

Alhadrami,

El-Din,

Hassan

et al. 2023

Pharmaceutics

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This study aimed to develop a self-nanoemulsifying drug delivery system (SNE) for sinapic acid (SA) to improve its solubility and antiviral activity. Optimal components for the SA-SNE formulation were selected, including Labrafil as the oil, Cremophor EL as the surfactant, and Transcutol as the co-surfactant. The formulation was optimized using surface response design, and the optimized SA-SNE formulation exhibited a small globule size of 83.6 nm, high solubility up to 127.1 ± 3.3, and a 100% transmittance. In vitro release studies demonstrated rapid and high SA release from the formulation. Pharmacokinetic analysis showed improved bioavailability by 2.43 times, and the optimized SA-SNE formulation exhibited potent antiviral activity against SARS-CoV-2. The developed SA-SNE formulation can enhance SA’s therapeutic efficacy by improving its solubility, bioavailability, and antiviral activity. Further in silico, modeling, and Gaussian accelerated molecular dynamics (GaMD)-based studies revealed that SA could interact with and inhibit the viral main protease (Mpro). This research contributes to developing effective drug delivery systems for poorly soluble drugs like SA, opening new possibilities for their application via nebulization in SARS-CoV-2 therapy.

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“…The KCZ-loaded liposomes were optimized by Box-Behnken design (BBD) using a using Design Expert® software. [15][16] A total of 17 runs (F1-F17) were created via software and investigated the effects of independent variables on response variables at three levels. Three independent variables selected were HSPC (X1), Cholesterol (X2), and, Soyabean oil (X3) whereas, % EE (Y1) and the vesicle size (PS; Y2).…”

Section: Formulation Optimizationmentioning

confidence: 99%

ph-Responsive Alendronic Acid-Coated Liposomes for Improved Treatment Osteosarcoma

Desai,

Manjappa,

Khulbe

2023

JAZ

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Objective Current research work aimed to develop pH-responsive osteosarcoma-targeted liposomes composed of non-oncology drugs previously identified for repositioning purposes. Material and Methods Using thin film hydration method, the Ketoconazole (KCZ)-, Simvastatin (SVN)-, and Niclosamide (NSD)-loaded non-targeted liposomes (KLs, SLs, and NLs respectively) were developed individually. The Aledronic acid-Choleteryl hemiscuccinate conjugate (AA-CHSC) was synthesized and confirmed using FTIR and 1H-NMR analysis. The AA-CHSC coated liposomes (pH sensitive and targeted liposome: PT-KLs, PT-SLs, and PT-NLs) were developed individually for the treatment of osteosarcoma with improved efficacy and reduced drug’s primary effects. The developed non-targeted and targeted liposomes were characterized for drug contentt,vesicle size, surface morphology using transmission electron microscope (TEM), in vitro pH-sensitive drug release behaviour using dialysis bag technique, and in vitro cytotoxicity characteristics against osteosarcoma cells. Results All non-targeted liposomes showed %drug content and mean vesicle size in the range of 41-75% and 161-182 nm, respectively. The AA-CHSC insertion into the liposomal membrane (targeted liposomes) has substantially improved the drug solubility in the membrane as a result of its amphiphilic nature. Furthermore, the targeted liposomes showed moderately increased mean vesicle size (203-210 nm) validating the surface modification. The TEM image revealed the formation of spherical, nearly spherical, and non-aggregated liposomes. The AA-CHSC insertion also caused liposomes sensitive to tumor pH (5.8); as a result, substantially higher drug release (58-80%) was observed as compared to non-targeted liposomes (34-52%). The cytotoxicity study results revealed substantially higher osteosarcoma cell (Saos-2) growth inhibition characteristics of targeted liposomes. Conclusions In conclusion, the developed targeted liposomes have potential application in the treatment of osteosarcoma. In addition, detailed anticancer activities should be revealed for the combination of targeted liposomes as the combination caused almost similar cytotoxicity as that of individual targeted liposomes.

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Oral self-emulsifying nanoemulsion systems for enhancing dissolution, bioavailability and anticancer effects of camptothecin

Cited by 10 publications

References 69 publications

Aceclofenac/Citronellol Oil Nanoemulsion Repurposing Study: Formulation, In Vitro Characterization, and In Silico Evaluation of Their Antiproliferative and Pro-Apoptotic Activity against Melanoma Cell Line

Aceclofenac/Citronellol Oil Nanoemulsion Repurposing Study: Formulation, In Vitro Characterization, and In Silico Evaluation of Their Antiproliferative and Pro-Apoptotic Activity against Melanoma Cell Line

Development and Evaluation of a Self-Nanoemulsifying Drug Delivery System for Sinapic Acid with Improved Antiviral Efficacy against SARS-CoV-2

ph-Responsive Alendronic Acid-Coated Liposomes for Improved Treatment Osteosarcoma

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