Prospectives of Solid Self-microemulsifying Systems in Novel Drug Delivery

Midha, Kanav; Nagpal, Manju; Singh, Garima; Aggarwal, Geeta

doi:10.2174/1567201813666160824123504

Cited by 16 publications

(9 citation statements)

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“… 20 Many techniques are used for converting liquid SNEDDS into S-SNEDDS such as spray drying, adsorption onto solid carriers, melt granulation, melt extrusion, and melt granulation. 21 The simplest way is the physical adsorption onto solid carriers as it involves the adsorption of liquid SNEDDS onto solid carriers by physical mixing to form free-flowing powders which can be filled into hard gelatin capsule or compressed into tablets after the addition of suitable excipients. 12 , 15 , 22 In recent years, porous carriers with large surface area as Aerosil ® 200 Pharma and Aeroperl ® 300 Pharma are used as solid carriers for the solidification of SNEDDS.…”

Section: Introductionmentioning

confidence: 99%

<p>Development, Characterization, and in-vivo Pharmacokinetic Study of Lamotrigine Solid Self-Nanoemulsifying Drug Delivery System</p>

Abdelmonem

Azer

Makky

et al. 2020

DDDT

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This study aimed to prepare solid self-nanoemulsified drug delivery system (S-SNEDDS) of lamotrigine (LMG) for enhancing its dissolution and oral bioavailability (BA). Methods: Nineteen liquid SNEDDS were prepared (R1-R19) using D-optimal design with different ratios of oil, surfactant (S), and cosurfactant (Cos). The formulations were characterized regarding robustness to dilution, droplet size, thermodynamic stability testing, selfemulsification time, in-vitro release in 0.1 N HCl and phosphate buffer (PB; pH 6.8). Design Expert ® 11 software was used to select the optimum formulations. Eight S-SNEDDS were prepared (S1-S8) using 2 3 factorial design, and characterized by differential scanning calorimetry (DSC), powder x-ray diffraction (PXRD), and scanning electron microscopy (SEM). The optimum formulation was chosen regarding in-vitro drug released in 0.1 N HCl and PB, compared to pure LMG and commercial tablet (Lamictal ®). The BA of LMG from the optimized S-SNEDDS formulation was evaluated in rabbits compared to pure LMG and Lamictal ®. Results: The optimized S-SNEDDS was S2, consisting of R9 adsorbed on Aeroperl ® 300 in a ratio of 1:1, with the best results regarding in-vitro drug released in 0.1 N HCl at 15 min (100%) compared to pure LMG (73.40%) and Lamictal ® (79.43%), and in-vitro drug released in PB at 45 min (100%) compared to pure LMG (30.46%) and Lamictal ® (92.08%). DSC, PXRD, and SEM indicated that LMG was molecularly dispersed within the solid nano-system. The BA of S2 was increased 2.03 and 1.605 folds compared to pure LMG, and Lamictal ® , respectively. Conclusion: S2 is a promising S-SNEDDS formulation. It can be a potential carrier for improving dissolution, and BA of LMG.

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Section: Introductionmentioning

confidence: 99%

<p>Development, Characterization, and in-vivo Pharmacokinetic Study of Lamotrigine Solid Self-Nanoemulsifying Drug Delivery System</p>

Abdelmonem

Azer

Makky

et al. 2020

DDDT

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“… Spontaneous formation  Ease of manufacture and low cost  Thermodynamic stability and improved solubilization of bioactive materials  More consistent temporal profiles of drug absorption Greater bioavailability  Less drug needs to be used  Faster release rates and improvement of the drug acceptance by consumers  Selective drug targeting toward a specific absorption window in the GI tract and  Drug protection from the hostile environment in the gut  They offer an improvement in the rate and extent of absorption and result in more reproducible blood time profiles  Lower cost. [47][48][49][50] SE Solid Dispersions: These formulations consist of a dispersion of the drug in an inert excipient matrix, but some manufacturing difficulties and stability problems existed. SE excipients have the ability to improve the absorption of drugs with poor solubility.…”

Section: Advantages Of S-smedds: 46mentioning

confidence: 99%

Untitled

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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“…In addition, precipitation of either active ingredient and/or oil constituents can also be influenced by storage temperature [14,15]. Therefore, attention has been given to transform liquid into solid SMEDDS by several techniques such as spray drying, spray cooling, super critical fluid technology, and using adsorption carriers [14,16]. Colloidal silica, a successful inexpensive hydrophobic carrier, requires common laboratory instruments to formulate as a vehicle for the preparation of solid SMEDDS [16,17].…”

Section: Introductionmentioning

confidence: 99%

“…Therefore, attention has been given to transform liquid into solid SMEDDS by several techniques such as spray drying, spray cooling, super critical fluid technology, and using adsorption carriers [14,16]. Colloidal silica, a successful inexpensive hydrophobic carrier, requires common laboratory instruments to formulate as a vehicle for the preparation of solid SMEDDS [16,17]. Carriers with absorbed SMEDDS are then compressed into tablets by wet granulation or direct compression methods [18,19].…”

Section: Introductionmentioning

confidence: 99%

Formulation Development of Albendazole-Loaded Self-Microemulsifying Chewable Tablets to Enhance Dissolution and Bioavailability

et al. 2019

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Albendazole is an anthelmintic agent with poor solubility and absorption. We developed a chewable tablet (200 mg drug equivalent), containing a self-microemulsifying drug delivery system (SMEDDS), with oral disintegrating properties. The emulsion was developed using sesame and soybean oils along with surfactant/co-surfactants, and the tablets were prepared by wet granulation using superdisintegrants and adsorbents. Infra-red (IR) spectral studies revealed no interaction between the drug and excipients, and all physical and chemical parameters were within acceptable limits. Stability studies for the formulation indicated no significant change over time. An in vitro release study indicated 100% drug release within 30 min, and in vivo plasma concentrations indicated that the area under the curve (AUC) of albendazole in rats administered SMEDDS chewable tablets was significantly higher than in those administered commercial tablets or powder (p-value < 0.05). The systemic bioavailability of albendazole achieved through the SMEDDS tablets was 1.3 times higher than that achieved by the administration of comparable quantities of albendazole commercial tablets. This was due to the higher dissolution of albendazole SMEDDS in the chewable tablets. We conclude that the SMEDDS chewable formulation can be used to improve the dissolution and systemic availability of poorly water-soluble drugs.

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Prospectives of Solid Self-microemulsifying Systems in Novel Drug Delivery

Cited by 16 publications

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<p>Development, Characterization, and in-vivo Pharmacokinetic Study of Lamotrigine Solid Self-Nanoemulsifying Drug Delivery System</p>

<p>Development, Characterization, and in-vivo Pharmacokinetic Study of Lamotrigine Solid Self-Nanoemulsifying Drug Delivery System</p>

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Formulation Development of Albendazole-Loaded Self-Microemulsifying Chewable Tablets to Enhance Dissolution and Bioavailability

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