An Improved Formulation Screening and Optimization Method Applied to the Development of a Self-Microemulsifying Drug Delivery System

Liu, Ying; Chen, Zhi Qiang; Zhang, Xin; Feng, Nian Ping; Zhao, Ji; Wu, Shan; Tan, Rong

doi:10.1248/cpb.58.16

Cited by 16 publications

(5 citation statements)

References 30 publications

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“…However, transdermal delivery by microemulsions was previously demonstrated to be safe for various drugs. [37][38][39][40] More animal results for the curcumin microemulsion are needed in order to evaluate whether the developed microemulsion is safe for the transdermal delivery of curcumin.…”

Section: Discussionmentioning

confidence: 99%

Development and Characterization of Eucalyptol Microemulsions for Topic Delivery of Curcumin

Liu

Chang

2011

Chem. Pharm. Bull.

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Transdermal drug delivery has many advantages over other administration routes: for example, avoidance of hepatic metabolism, convenient administration for the patient, and easy withdrawal of treatment if necessary. Despite extensive studies of transdermal drug delivery, only a few drug formulations are commercially available. 1) One of the reasons for this is the permeation barrier by the stratum corneum to exogenous substances. Skin penetration enhancement can be chieved using appropriate physical and chemical means to overcome the skin's barrier function. Chemical penetration enhancers such as fatty acids, fatty esters, surfactants, and terpenes have received considerable attention due to their low cost, ease of use, safety, and efficacy.2) Terpenes are lipophilic ingredients of essential oils which can disturb intracellular lipids and increase the fluidization of the stratum corneum, thereby enhancing drug penetration.3) Eucalyptus oil (eucalyptol, a terpene from trees) was adopted as the oil phase to design transdermal vehicles for various drugs including estradiol, progesterone, cyproterone acetate, finasteride, and hydrocortisone. 4,5) Investigations of microemulsions composed by eucalyptus/peppermint oil and water were reported to have many potential applications.6,7) Lipid-based systems such as microemulsions, nanoemulsions, solid lipid nanoparticles, and liposomes were recently applied to transdermal drug delivery. 8) Microemulsions are single phase, optically isotropic nano-structured solutions composed of a surfactant, cosurfactant, oil, and water. The ability of microemulsions to deliver drugs through a transdermal route in a controlled manner was recently reviewed. 9) Advantages of microemulsion delivery systems include spontaneous formation, easy preparation, low viscosity, high surface area, high drug solubilization, optical transparency, and thermodynamic stability.10) Microemulsions were applied to deliver different lipophilic drugs including fluconazole, 11) penciclovir, 12) quercetin, 13) diclofenac, 14) and progesterone 15) through the transdermal route. Those in vitro and in vivo studies demonstrated that lipophilic drugs incorporated into microemulsions can efficiently penetrate the skin.Curcumin and curcuminoids are yellow polyphenolic compounds extracted from the spice turmeric (Curcuma longa). Recent studies demonstrated that curcumin has the potential to protect skin by reducing inflammation through nuclear factor (NF)-kB inhibition and to reduce wound-healing time by improving collagen deposition.16) Curcumin can regenerate muscle cells after traumatic injury by modulating NF-kB activity within muscle tissues. Additionally, the use of curcumin for the chemoprevention and treatment of various skin diseases like scleroderma, psoriasis, and skin cancer was reviewed.16) Patel et al. demonstrated that curcumin-containing films have good anti-inflammatory activity against carrageenan-induced edema in rats similar to a standard formulation through the transdermal route.17) Those studies sugg...

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Section: Discussionmentioning

confidence: 99%

Development and Characterization of Eucalyptol Microemulsions for Topic Delivery of Curcumin

Liu

Chang

2011

Chem. Pharm. Bull.

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“…The accumulated amount of drug released from the SMEDDS in 120 min was approximately 90%, as opposed to 35% from suspension. The results showed that SMEDDS released faster than suspension [ 139 ].…”

Section: Strategies To Improve Solubility and Bioavailabilitymentioning

confidence: 99%

Novel Strategies for Solubility and Bioavailability Enhancement of Bufadienolides

Shao

et al. 2021

Molecules

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Toad venom contains a large number of bufadienolides, which have a variety of pharmacological activities, including antitumor, cardiovascular, anti-inflammatory, analgesic and immunomodulatory effects.. The strong antitumor effect of bufadienolides has attracted considerable attention in recent years, but the clinical application of bufadienolides is limited due to their low solubility and poor bioavailability. In order to overcome these shortcomings, many strategies have been explored, such as structural modification, solid dispersion, cyclodextrin inclusion, microemulsion and nanodrug delivery systems, etc. In this review, we have tried to summarize the pharmacological activities and structure–activity relationship of bufadienolides. Furthermore, the strategies for solubility and bioavailability enhancement of bufadienolides also are discussed. This review can provide a basis for further study on bufadienolides.

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“…A wide variation was seen among the observed response indicating that the independent variables had significant effect on dependent variables. For further statistical analysis, the three responses were individually fitted to the second-order polynomial model and each model was validated by analysis of variance combined with the F test (26,27). As shown in Table III, the independent variables had significant effect (p value <0.05) for all the response variables.…”

Section: Plackett-burman Screening Designmentioning

confidence: 99%

Design, Optimization, and Evaluation of Lurasidone Hydrochloride Nanocrystals

et al. 2015

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Abstract. The present investigation was carried out to design, optimize, and evaluate lurasidone hydrochloride nanocrystals for improving its solubility and dissolution characteristics. Nanocrystals were prepared by media milling technique using zirconium oxide beads with 0.1 mm diameter. Various stabilizers, viz. poloxamer 188, PVP K30, SLS, HPMC E15, and PVP S 630 D, were evaluated to stabilize the nanocrystals. The Pareto chart obtained through Plackett-Burman screening design revealed that HPMC E 15 showed the highest standardized effect (p value <0.05) on percent dissolution efficiency at 2 min. In subsequent studies, a 3 2 factorial design was employed to quantify the effect of two independent variables, namely amount of stabilizer and milling time on predetermined response variables mean particle size, saturation solubility, and percent dissolution efficiency at 2 min. Statistical analysis of the factorial design revealed that all predetermined response variables were significantly dependent (p value <0.05) on the independent variables. The observed response of the optimized batch prepared as per the desirability function was in close agreement with predicted response, and mathematical model generated was validated. The optimized batch was lyophilized, and X-ray powder diffraction studies indicated that there was no substantial change in crystallinity of the drug. The optimized formulation showed mean particle size of 228 nm and released almost all the drug within first 5 min. Since the crystallinity of the drug is maintained, improvement in saturation solubility and dissolution efficiency could be attributed to decrease in mean particle size of the drug.

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An Improved Formulation Screening and Optimization Method Applied to the Development of a Self-Microemulsifying Drug Delivery System

Cited by 16 publications

References 30 publications

Development and Characterization of Eucalyptol Microemulsions for Topic Delivery of Curcumin

Development and Characterization of Eucalyptol Microemulsions for Topic Delivery of Curcumin

Novel Strategies for Solubility and Bioavailability Enhancement of Bufadienolides

Design, Optimization, and Evaluation of Lurasidone Hydrochloride Nanocrystals

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