Self-emulsifying therapeutic system: a potential approach for delivery of lipophilic drugs

Wadhwa, Jyoti; Nair, Anroop B.; Kumria, Rachna

doi:10.1590/s1984-82502011000300003

Cited by 28 publications

(17 citation statements)

References 87 publications

(74 reference statements)

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“…Preliminary studies were carried out to select ingredients for preparing moxifloxacin nanoemulsion. Indeed, the selection of the vehicle is extremely important as it provides good solubilizing efficiency of the drug, which is essential for constituting a nanoemulsion [24]. Hence, the solubility of moxifloxacin in various oils, surfactants, and cosurfactants was determined by the standard procedures.…”

Section: Resultsmentioning

confidence: 99%

Nanoemulsion Based Vehicle for Effective Ocular Delivery of Moxifloxacin Using Experimental Design and Pharmacokinetic Study in Rabbits

et al. 2019

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Nanoemulsion is one of the potential drug delivery strategies used in topical ocular therapy. The purpose of this study was to design and optimize a nanoemulsion-based system to improve therapeutic efficacy of moxifloxacin in ophthalmic delivery. Moxifloxacin nanoemulsions were prepared by testing their solubility in oil, surfactants, and cosurfactants. A pseudoternary phase diagram was constructed by titration technique and nanoemulsions were obtained with four component mixtures of Tween 80, Soluphor® P, ethyl oleate and water. An experiment with simplex lattice design was conducted to assess the influence of formulation parameters in seven nanoemulsion formulations (MM1–MM7) containing moxifloxacin. Physicochemical characteristics and in vitro release of MM1–MM7 were examined and optimized formulation (MM3) was further evaluated for ex vivo permeation, antimicrobial activity, ocular irritation and stability. Drug pharmacokinetics in rabbit aqueous humor was assessed for MM3 and compared with conventional commercial eye drop formulation (control). MM3 exhibited complete drug release in 3 h by Higuchi diffusion controlled mechanism. Corneal steady state flux of MM3 (~32.01 µg/cm2/h) and control (~31.53 µg/cm2/h) were comparable. Ocular irritation study indicated good tolerance of MM3 and its safety for ophthalmic use. No significant changes were observed in the physicochemical properties of MM3 when stored in the refrigerator for 3 months. The greater aqueous humor concentration (Cmax; 555.73 ± 133.34 ng/mL) and delayed Tmax value (2 h) observed in MM3 suggest a reduced dosing frequency and increased therapeutic efficacy relative to control. The area under the aqueous humor concentration versus time curve (AUC0–8 h) of MM3 (1859.76 ± 424.51 ng·h/mL) was ~2 fold higher (p < 0.0005) than the control, suggesting a significant improvement in aqueous humor bioavailability. Our findings suggest that optimized nanoemulsion (MM3) enhanced the therapeutic effect of moxifloxacin and can therefore be used as a safe and effective delivery vehicle for ophthalmic therapy.

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Section: Resultsmentioning

confidence: 99%

Nanoemulsion Based Vehicle for Effective Ocular Delivery of Moxifloxacin Using Experimental Design and Pharmacokinetic Study in Rabbits

et al. 2019

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“…The formulation was developed using the excipients that showed the highest solubilizing capacity for the drug: Plurol ® oleique CC497, Labrasol ® and Transcutol ® P ( Figure 2 ). The search for the most suitable components with regards to the solubility of the drug is a critical step in the development of a ME in order to ensure its stability and high drug loading capacity [ 40 , 41 ]. Labrasol ® is a non-ionic oil/water surfactant characterized by its low irritability for the skin and which is commonly used with Plurol ® oleique in dermal formulations [ 42 ].…”

Section: Discussionmentioning

confidence: 99%

Apremilast Microemulsion as Topical Therapy for Local Inflammation: Design, Characterization and Efficacy Evaluation

et al. 2020

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Apremilast (APR) is a selective phosphodiesterase 4 inhibitor administered orally in the treatment of moderate-to-severe plaque psoriasis and active psoriatic arthritis. The low solubility and permeability of this drug hinder its dermal administration. The purpose of this study was to design and characterize an apremilast-loaded microemulsion (APR-ME) as topical therapy for local skin inflammation. Its composition was determined using pseudo-ternary diagrams. Physical, chemical and biopharmaceutical characterization were performed. Stability of this formulation was studied for 90 days. Tolerability of APR-ME was evaluated in healthy volunteers while its anti-inflammatory potential was studied using in vitro and in vivo models. A homogeneous formulation with Newtonian behavior and droplets of nanometric size and spherical shape was obtained. APR-ME released the incorporated drug following a first-order kinetic and facilitated drug retention into the skin, ensuring a local effect. Anti-inflammatory potential was observed for its ability to decrease the production of IL-6 and IL-8 in the in vitro model. This effect was confirmed in the in vivo model histologically by reduction in infiltration of inflammatory cells and immunologically by decrease of inflammatory cytokines IL-8, IL-17A and TNFα. Consequently, these results suggest that this formulation could be used as an attractive topical treatment for skin inflammation.

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“…The intestinal hydrolysis of prodrug by cholinesterase can be protected if polysorbate 20 is an emulsifier in microemulsion formulation . These systems are formed spontaneously without aid of energy or heating 19, thus suitable for thermolabile drugs such as peptides.…”

Section: Reduction In Inter-subject and Intra-subjectmentioning

confidence: 99%

“…The surface-active agents are amphiphilic by nature, the usual surfactant concentration in self-emulsifying formulations required to form and maintain an emulsion state in the GI tract ranged from 30 to 60% w/w of the formulation. The most widely recommended ones being the non-ionic surfactants with a relatively high (HLB) hydrophilic-lipophilic balance 18,19,20 .…”

Section: Surfactantsmentioning

confidence: 99%

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2020

IJPSR

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Oral route has always been the preferred route of drug administration in many diseases. This route is limited to those drugs molecules that are permeable across the gastric mucosa and are sparingly soluble. Solubility is an important parameter to achieve the desired concentration of drug in systemic circulation for therapeutic response. As a consequence of modern drug discovery techniques, there has been a steady increase in the number of new active lipophilic compounds that are poorly water-soluble. It is a challenge for a scientist to convert those molecules into an orally administered formulation with sufficient bioavailability. Improving oral bioavailability of poorly watersoluble drugs using self micro emulsifying drug delivery systems (SMEDDS) appears most promising. Currently, various technologies are available to deal with insoluble drugs such as micronization, solid dispersions, complex formation, etc. Among the several approaches, SMEDDS has emerged as a distinctive approach used to improve the bioavailability of hydrophobic drugs. SMEDDS is isotropic mixture of drug, surfactants, cosurfactants, and oil which have unique ability to form fine o/w microemulsion on slight shaking followed by dilution with gastrointestinal fluid. In-vitro features such as concentration of surfactants, ratio of oil to surfactant, zeta potential, and size of droplet play a crucial role in drug absorption orally. The present article compiled comprehensively which gives a complete overview of SMEDDS as a promising approach to effectively tackle the problem of poorly soluble molecules. It also provides a discussion on recent developments in SMEDDS and solid SMEDDS, their characterization and applications. INTRODUCTION: As a consequence of modern drug discovery techniques, there has been a steady increase in the number of new pharmacologically active lipophilic compounds that are poorly watersoluble. About 40% of new drugs exhibit poor water solubility, resulting in lack of dose proportionality, high inter-and intra-subject variability, and low oral bioavailability.

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Self-emulsifying therapeutic system: a potential approach for delivery of lipophilic drugs

Cited by 28 publications

References 87 publications

Nanoemulsion Based Vehicle for Effective Ocular Delivery of Moxifloxacin Using Experimental Design and Pharmacokinetic Study in Rabbits

Nanoemulsion Based Vehicle for Effective Ocular Delivery of Moxifloxacin Using Experimental Design and Pharmacokinetic Study in Rabbits

Apremilast Microemulsion as Topical Therapy for Local Inflammation: Design, Characterization and Efficacy Evaluation

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