Lipid based nanocarriers: A novel paradigm for topical antifungal therapy

Nene, Shweta; Shah, Saurabh; Rangaraj, Nagarjun; Mehra, Neelesh Kumar; Singh, Pankaj Kumar; Srivastava, Saurabh

doi:10.1016/j.jddst.2021.102397

Cited by 32 publications

(34 citation statements)

References 214 publications

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“…Of these nano-carriers, lipid-based type is the most common in pharmaceutical research. 2 These lipid-based nano-carriers can be subdivided into three different classes: vesicular carriers such as liposomes, 3 niosomes, 4 proniosomes, 5 cerosomes, 6 nano-particulate carriers 7 , 8 and emulsion based carriers. 9–11 …”

Section: Introductionmentioning

confidence: 99%

Statistical Sequential Experimentation: Preliminary Mixed Factorial Design, I-Optimal Mixture Design Then Finally Novel Design Space Expansion for Optimization of Tazarotene Cubosomes

Hegazy¹,

Tag²,

Habib³

2022

IJN

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Objective This study aims to illustrate the potential of sequential experimentation for statistically scientific based optimization of Tazarotene (TAZA) cubosomes. Methods Hot melt emulsification method was used for cubosomes preparation. A preliminary (3.2) mixed factorial design (MFD) was conducted to choose suitable types of stabilizer and surfactant that maximize entrapment efficiency (EE) and minimize particle size (PS). These chosen stabilizer and surfactant were to be used in the statistical design proposed for optimization of TAZA cubosomes (I-optimal mixture design) (IOMD). Glyceryl monooleate (GMO), stabilizer and surfactant amounts were the three mixture components (MixCs) studied in that design. Responses (EE, PS and drug percent released after 24 hours (Q24h)) were statistically analyzed. Numerical optimization using desirability function based on different responses’ importance was used to find an IOMD-optimized formulation (IOMD-OF) with the predetermined characters. Then, a novel statistical methodology of design space expansion was adopted to enhance Q24h. Suitable models to express EE, PS and Q24h were elucidated over the expanded mixture design (EMD) space. Validity of derived models was verified via prediction intervals and percent deviations of actual values from predicted ones for all the EMD design points. EMD was then navigated to find EMD-OF. Results Analysis of MFD showed that Pluronic-F68 and polyvinyl alcohol were the best stabilizer and surfactant to be used. First stage optimization after IOMD analysis led to a formulation with unsatisfactory Q24h of 58.8%. After design space expansion adoption, re-analysis and re-optimization, a satisfactory EMD-OF having EE of 82.1%, PS of 273.0 nm and Q24h of 68.8% was found. Conclusion Statistical sequential experimentation with the novel design space expansion approach proved to be a successful paradigm for enhancing TAZA cubosomes optimization. Thus, this paradigm is expected to have promising future applications in various pharmaceutical formulations optimization.

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Section: Introductionmentioning

confidence: 99%

Statistical Sequential Experimentation: Preliminary Mixed Factorial Design, I-Optimal Mixture Design Then Finally Novel Design Space Expansion for Optimization of Tazarotene Cubosomes

Hegazy¹,

Tag²,

Habib³

2022

IJN

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“…First, due to their ability to reduce surface tension, they increase fluidity and solubilize and extract lipids from the epidermis. They can also lead to corneocyte disruption through binding and interaction with keratin filaments [153]. Secondly, the adhesion of niosomes to the skin surface causes changes of the SC properties by reducing water loss from the epidermis.…”

Section: Niosomesmentioning

confidence: 99%

“…Depending on the target or on the encapsulated substance, the composition can be modified, and this directly affects the transfersome properties. The easiest way to change the transfersome properties is to vary the ratio of components and type of surfactant [153]. For example, 12 systems with different surfactants, drug: phosphatidylcholine and surfactant:phosphatidylcholine ratios were studied in [180].…”

Section: Transfersomes and Transethosomesmentioning

confidence: 99%

“…Transethosomes consist of phospholipid, ethanol, water and edge activator (Tween 20, Tween 80, Span 20, sodium taurocholate, sodium deoxycholate) or permeation enhancer (for instance, oleic acid). The issue of transethosomes was raised in several reviews [153,172,201,202]. In our review, we will focus on in vivo experiments with transethosomes.…”

Section: Transfersomes and Transethosomesmentioning

confidence: 99%

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Self-Assembling Drug Formulations with Tunable Permeability and Biodegradability

et al. 2021

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This review focuses on key topics in the field of drug delivery related to the design of nanocarriers answering the biomedicine criteria, including biocompatibility, biodegradability, low toxicity, and the ability to overcome biological barriers. For these reasons, much attention is paid to the amphiphile-based carriers composed of natural building blocks, lipids, and their structural analogues and synthetic surfactants that are capable of self-assembly with the formation of a variety of supramolecular aggregates. The latter are dynamic structures that can be used as nanocontainers for hydrophobic drugs to increase their solubility and bioavailability. In this section, biodegradable cationic surfactants bearing cleavable fragments are discussed, with ester- and carbamate-containing analogs, as well as amino acid derivatives received special attention. Drug delivery through the biological barriers is a challenging task, which is highlighted by the example of transdermal method of drug administration. In this paper, nonionic surfactants are primarily discussed, including their application for the fabrication of nanocarriers, their surfactant-skin interactions, the mechanisms of modulating their permeability, and the factors controlling drug encapsulation, release, and targeted delivery. Different types of nanocarriers are covered, including niosomes, transfersomes, invasomes and chitosomes, with their morphological specificity, beneficial characteristics and limitations discussed.

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“…In recent years, microemulsion (ME) has gathered a lot of importance as an efficient drug delivery vehicle. The existence of compartmentalized hydrophobic and lipophilic domains aids in the incorporation of polar and non-polar components [11]. MEs are optically transparent, thermodynamically stable, and have low viscous colloidal dispersion of oil and aqueous phase stabilized by a surfactant, sometimes in combination with cosurfactant [12].…”

Section: Introductionmentioning

confidence: 99%

Synergistic antifungal potential of fluconazole-based cardamom oil oral microemulsion formulation against C. albicans

TIWARI¹,

SIVAKUMAR²

2022

jrp

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Microemulsion has grabbed a lot of attention in the last few decades as a unique candidate for drug delivery owing to its low viscosity, limpidness, ease of preparation, and good thermodynamic stability. The potential to incorporate drugs from unlike lipophilicity and its spontaneous formation makes it a suitable candidate for pharmaceutical application. The objective of the current study is to enhance the solubility of Fluconazole, an antifungal drug by formulating a microemulsion made up of cardamom oil, tween 20, and water (5:15:80). The formulations were checked for their physiochemical properties and thermodynamic stability. An antimicrobial activity like zone of inhibition, minimum inhibitory concentration and kill kinetics assay for optimized formulations were checked against C. albicans. The droplet size of the system and FLZ loaded microemulsion was found to be 7.8 and 8.6nm respectively. In vitro drug release from optimized microemulsion formulation showed efficient release (78.45%) compared to the bulk API (7.98%) in simulated intestinal fluid. The cytoplasmic release for CDMM FLZ ME at 0.5X, 1X and 5X was 43.24%, 82.11%, 91.73% respectively. In vitro toxicity demonstrated a lower toxicity rate with lower surfactant concentration against human lymphocytes and its safer usage. SEM analysis depicts the morphological distortion in C. albicans that occurred due to the interaction with microemulsion. The results indicate cardamom oil-based microemulsion is an efficient drug delivery vehicle intended for oral usage.

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Lipid based nanocarriers: A novel paradigm for topical antifungal therapy

Cited by 32 publications

References 214 publications

Statistical Sequential Experimentation: Preliminary Mixed Factorial Design, I-Optimal Mixture Design Then Finally Novel Design Space Expansion for Optimization of Tazarotene Cubosomes

Statistical Sequential Experimentation: Preliminary Mixed Factorial Design, I-Optimal Mixture Design Then Finally Novel Design Space Expansion for Optimization of Tazarotene Cubosomes

Self-Assembling Drug Formulations with Tunable Permeability and Biodegradability

Synergistic antifungal potential of fluconazole-based cardamom oil oral microemulsion formulation against C. albicans

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