Formulation and in vitro evaluation of pH-responsive ethosomes for vaginal delivery of metronidazole

Mbah, Chukwuemeka C.; Builders, Philip F.; Nzekwe, Ifeanyi T.; Kunle, Olobayo O.; Adikwu, M. U.; Attama, AA

doi:10.1016/s1773-2247(14)50120-7

Cited by 25 publications

(7 citation statements)

References 27 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The increase in phospholipid concentration will provide more vesicles, thus supplying more opportunities for PF to encapsulate into the inner water phase enclosed by the phospholipid bilayer membrane and enhancing the EE. 38 Cholesterol in the phospholipid bilayer acted as a membrane-rigidifying agent, and it had a significant effect on the PDI of glycerosomes in this study. This effect may be connected with the ability of cholesterol to stabilize the lipid bilayer and to ensure that the vesicles are uniformly distributed in the water medium.…”

Section: Discussionmentioning

confidence: 56%

Essential oil-mediated glycerosomes increase transdermal paeoniflorin delivery: optimization, characterization, and evaluation in vitro and in vivo

Zhang

et al. 2017

IJN

View full text Add to dashboard Cite

In this study, a novel glycerosome carrier containing essential oils was prepared for topical administration of paeoniflorin (PF) to enhance its transdermal drug delivery and improve drug absorption in the synovium. The formulation of glycerosomes was optimized by a uniform design, and the final vehicle was composed of 5% (w/v) phospholipid, 0.6% (w/v) cholesterol, and 10% (v/v) glycerol, with 2% (v/v) Speranskia tuberculata essential oil (STO) as the transdermal enhancer. The in vitro transdermal flux of PF loaded in the STO-glycerosomes was 1.4-fold, 1.6-fold, and 1.7-fold higher than those of glycerosomes, liposomes, and tinctures, respectively. In vivo studies showed that the use of STO-glycerosomes was associated with a 3.1-fold greater accumulation of PF in the synovium than that of common glycerosomes. This finding was confirmed by in vivo imaging studies, which found that the fluorescence intensity of Cy5.5-loaded STO-glycerosomes in mice knee joints was 1.8-fold higher than that of the common glycerosomes 5 h after administration. The glycerosomes mediated by STO exhibited considerable skin permeability as well as improved drug absorption in the synovium, indicating that STO-glycerosomes may be a potential PF transdermal delivery vehicle for the treatment of rheumatoid arthritis caused by synovium lesions.

show abstract

Section: Discussionmentioning

confidence: 56%

Essential oil-mediated glycerosomes increase transdermal paeoniflorin delivery: optimization, characterization, and evaluation in vitro and in vivo

Zhang

et al. 2017

IJN

View full text Add to dashboard Cite

show abstract

“…116 Chang et al studied the ability of ethosomes and liposomes to enhance the oral bioavailability and tissue distribution of silymarin in an in vivo study. Pharmacokinetic results revealed that both vesicular systems (ie, ethosomes and liposomes) were able to improve the bioavailability of silymarin, but better results were gained from liposomes.…”

Section: Ethosomal Systems For Other Administrationsmentioning

confidence: 99%

“…The ethosomal gel demonstrated sustained delivery of metronidazole, with a maximum flux of 143.67±2.73 µg/cm 2 /h. 116 However, in vivo studies are required to evaluate the suitability of ethosomal systems for this route of administration.…”

Section: Ethosomal Systems For Other Administrationsmentioning

confidence: 99%

Ethosomal nanocarriers: the impact of constituents and formulation techniques on ethosomal properties, in vivo studies, and clinical trials

Abdulbaqi

Darwis

Khan

et al. 2016

IJN

314

215

View full text Add to dashboard Cite

Ethosomal systems are novel lipid vesicular carriers containing a relatively high percentage of ethanol. These nanocarriers are especially designed for the efficient delivery of therapeutic agents with different physicochemical properties into deep skin layers and across the skin. Ethosomes have undergone extensive research since they were invented in 1996; new compounds were added to their initial formula, which led to the production of new types of ethosomal systems. Different preparation techniques are used in the preparation of these novel carriers. For ease of application and stability, ethosomal dispersions are incorporated into gels, patches, and creams. Highly diverse in vivo models are used to evaluate their efficacy in dermal/transdermal delivery, in addition to clinical trials. This article provides a detailed review of the ethosomal systems and categorizes them on the basis of their constituents to classical ethosomes, binary ethosomes, and transethosomes. The differences among these systems are discussed from several perspectives, including the formulation, size, ζ-potential (zeta potential), entrapment efficiency, skin-permeation properties, and stability. This paper gives a detailed review on the effects of ethosomal system constituents, preparation methods, and their significant roles in determining the final properties of these nanocarriers. Furthermore, the novel pharmaceutical dosage forms of ethosomal gels, patches, and creams are highlighted. The article also provides detailed information regarding the in vivo studies and clinical trials conducted for the evaluation of these vesicular systems.

show abstract

“…Mistry and Ravikumar reported that the cold method produces azelaic ethosomes with an entrapment efficiency of 35-43% which was lower than that resulting from the thin-layer hydration method (55-88%) [5]. Mbah et al prepared metronidazole ethosomes using the thin-layer hydration method with an entrapment efficiency of 50.31±3.38%, average particle size of 179.9 nm, and a polydispersity index (PDI) of 0.338 [6]. Linoleic acid ethosomes prepared using the cold method had an entrapment efficiency of 64.37±5.91%, average particle size of 343.10±32.49 nm, and a PDI of 0.105±0.012 [7].…”

Section: Introductionmentioning

confidence: 99%

Preparation and Characterization of Anti-Acne Ethosomes Using Cold and Thin-Layer Hydration Methods

Mustofa

Iskandarsyah

2018

Int J App Pharm

View full text Add to dashboard Cite

Objective: This study aimed to prepare and characterize anti-acne ethosomes using the cold-and thin-layer hydration methods.Methods: A sonication step was included during ethosome preparation to improve the quality of the cold method. Azelaic acid, Phospholipon 90G, ethanol, propylene glycol, and phosphate buffer (pH 7.4) were used in the procedures. Prepared ethosomal suspensions were characterized using transmission electron microscopy, particle-size analysis, and spectrophotometry.Results: Ethosomes prepared using the thin-layer hydration method (F1) had small unilamellar vesicles, while those prepared using the cold method with 15-min sonication (F4) showed spherical, elliptical, unilamellar, and multilamellar vesicles. F1 ethosomes had a D mean volume of 648.57±231.26, whereas those prepared using the cold method with 5-(F2), 10-(F3), and 15-min (F4) sonication had D mean volumes of 2734.04±231.49 nm, 948.90±394.52 nm, and 931.69±471.84 nm, respectively. Polydispersity indices of F2, F3, and F4 ethosomes were 0.74±0.21, 0.86±0.05, and 0.91±0.03, respectively, with a poor particle-size distribution, compared to that of F1 (0.39±0.01). Zeta potentials of F1-F4 ethosomes were −38.27±1.72 mV, −23.53±1.04 mV, −31.4±1.04 mV, and −34.3±1.61 mV, respectively. Entrapment efficiencies of F1-F4 ethosomes were 90.71±0.11%, 53.84±3.16%, 72.56±0.28%, and 75.11±1.42%, respectively. Conclusion:Anti-acne ethosomes produced using the thin-layer hydration method had superior properties than those produced using the cold method with 15-min sonication.

show abstract

Formulation and in vitro evaluation of pH-responsive ethosomes for vaginal delivery of metronidazole

Cited by 25 publications

References 27 publications

Essential oil-mediated glycerosomes increase transdermal paeoniflorin delivery: optimization, characterization, and evaluation in vitro and in vivo

Essential oil-mediated glycerosomes increase transdermal paeoniflorin delivery: optimization, characterization, and evaluation in vitro and in vivo

Ethosomal nanocarriers: the impact of constituents and formulation techniques on ethosomal properties, in vivo studies, and clinical trials

Preparation and Characterization of Anti-Acne Ethosomes Using Cold and Thin-Layer Hydration Methods

Contact Info

Product

Resources

About