A COMPREHENSIVE REVIEW ON SUPERSATURABLE SELF-NANOEMULSIFYING DRUG DELIVERY SYSTEM

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2021.v14i8.41987 ◽

2021 ◽

pp. 40-44

Author(s):

MUTHADI RADHIKA REDDY ◽

KUMAR SHIVA GUBBIYAPPA

Keyword(s):

Drug Delivery ◽

Drug Delivery Systems ◽

Delivery Systems ◽

Water Soluble ◽

In Vitro Tests ◽

Drug Bioavailability ◽

Advantages And Disadvantages ◽

Anti Cancer

Lipid-based drug delivery systems are extensively reported in the literature for enhancing drug solubility, permeability, and bioavailability. Self-nanoemulsifying drug delivery systems (SNEDDS) are a superior strategy for enhancing solubility and bioavailability of poorly water-soluble compounds and the most prevailing and commercially viable oil-based approach for drugs that exhibit low dissolution rate and inadequate absorption. However, these formulations have few limitations that include in vivo drug precipitation, inferior in vitro in vivo correlation owing to unavailability of in vitro tests, handling issues of liquid formulation, and physicochemical instability of drugs. These limitations are overcome by potential systems such as supersaturable SNEDDS (S-SNEDDS) which are prepared by addition of precipitation inhibitors into formulated SNEDDS to maintain drug supersaturation post dispersion in gastrointestinal tract. These systems improve drug bioavailability and reduce the inconsistency of exposure. In addition, these formulations also help to overcome the drawbacks of liquid and capsule dosage forms. The S-SNEDDS provides an effective approach for improving the dissolution and bioavailability of anti-cancer agents. In this article, an attempt was made to present an overview of SNEDDS, S-SNEDDS, their mechanism, formulation excipients, recent advancements, advantages, and disadvantages of SNEDDS formulations. The article also focuses on reviewing the application of S-SNEDDS in enhancing the solubility and bioavailability of anti-cancer drugs in cancer therapy.

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Current Status of Supersaturable Self-Emulsifying Drug Delivery Systems

Pharmaceutics ◽

10.3390/pharmaceutics12040365 ◽

2020 ◽

Vol 12 (4) ◽

pp. 365 ◽

Cited By ~ 2

Author(s):

Heejun Park ◽

Eun-Sol Ha ◽

Min-Soo Kim

Keyword(s):

Drug Delivery ◽

Drug Delivery Systems ◽

Drug Application ◽

In Vitro Digestion ◽

Delivery Systems ◽

Water Soluble ◽

Current Status ◽

In Vitro Tests

Self-emulsifying drug delivery systems (SEDDSs) are a vital strategy to enhance the bioavailability (BA) of formulations of poorly water-soluble compounds. However, these formulations have certain limitations, including in vivo drug precipitation, poor in vitro in vivo correlation due to a lack of predictive in vitro tests, issues in handling of liquid formulation, and physico-chemical instability of drug and/or vehicle components. To overcome these limitations, which restrict the potential usage of such systems, the supersaturable SEDDSs (su-SEDDSs) have gained attention based on the fact that the inclusion of precipitation inhibitors (PIs) within SEDDSs helps maintain drug supersaturation after dispersion and digestion in the gastrointestinal tract. This improves the BA of drugs and reduces the variability of exposure. In addition, the formulation of solid su-SEDDSs has helped to overcome disadvantages of liquid or capsule dosage form. This review article discusses, in detail, the current status of su-SEDDSs that overcome the limitations of conventional SEDDSs. It discusses the definition and range of su-SEDDSs, the principle mechanisms underlying precipitation inhibition and enhanced in vivo absorption, drug application cases, biorelevance in vitro digestion models, and the development of liquid su-SEDDSs to solid dosage forms. This review also describes the effects of various physiological factors and the potential interactions between PIs and lipid, lipase or lipid digested products on the in vivo performance of su-SEDDSs. In particular, several considerations relating to the properties of PIs are discussed from various perspectives.

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Effects of Hydrophilic Carriers on Structural Transitions and In Vitro Properties of Solid Self-Microemulsifying Drug Delivery Systems

Pharmaceutics ◽

10.3390/pharmaceutics11060267 ◽

2019 ◽

Vol 11 (6) ◽

pp. 267 ◽

Cited By ~ 5

Author(s):

Tao Yi ◽

Jifen Zhang

Keyword(s):

Drug Delivery ◽

Drug Delivery Systems ◽

Delivery Systems ◽

Water Soluble ◽

Drug Dissolution ◽

Commercial Application ◽

Simulated Gastric Fluid ◽

Structural Transitions

Self-microemulsifying drug delivery systems (SMEDDS) offer potential for improving the oral bioavailability of poorly water-soluble drugs. However, their susceptibilities during long term storage and in vivo precipitation issues limit their successful commercial application. To overcome these limitations, SMEDDS can be solidified with solid carriers, thus producing solid self-microemulsifying drug delivery systems (S-SMEDDS). In this study, effects of various hydrophilic carriers on structural transitions and in vitro properties of S-SMEDDS were investigated in order to set up in vitro methods for screening out appropriate carriers for S-SMEDDS. Liquid SMEDDS was prepared and characterized using nimodipine as a model drug. The effects of various hydrophilic carriers on internal microstructure and solubilization of SMEDDS were investigated by conductivity measurement and in vitro dispersion test. The results showed that hydrophilic carriers including dextran 40, maltodextrin and PVP K30 seemed to delay the percolation transition of SMEDDS, allowing it to maintain a microstructure that was more conducive to drug dissolution, thus significantly increasing the solubilization of nimodipine in the self-microemulsifying system and decreasing drug precipitation when dispersed in simulated gastric fluid. S-SMEDDS of nimodipine were prepared by using spray drying with hydrophilic carriers. The effects of various hydrophilic carriers on in vitro properties of S-SMEDDS were investigated by using SEM, DSC, PXRD and in vitro dissolution. The results showed that properties of hydrophilic carriers, especially relative molecular mass of carriers, had obvious influences on surface morphologies of S-SMEDDS, reconstitution of microemulsion and physical state of nimodipine in S-SMEDDS. Considering that in vitro properties of S-SMEDDS are closely related to their pharmacokinetic properties in vivo, the simple and economical in vitro evaluation methods established in this paper can be used to screen solid carriers of S-SMEDDS well.

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Inorganic-organic Nanomaterials for Therapeutics and Molecular Imaging Applications

Nanoscience &Nanotechnology-Asia ◽

10.2174/2210681209666190807145229 ◽

2020 ◽

Vol 10 (6) ◽

pp. 748-765

Author(s):

Alaa A.A. Aljabali ◽

Mohammad A. Obeid

Keyword(s):

Drug Delivery ◽

Drug Delivery Systems ◽

Delivery Systems ◽

Cell Labeling ◽

Bibliographic Databases ◽

Medical Applications ◽

Advantages And Disadvantages ◽

Naturally Occurring

Background:: Surface modification of nanoparticles with targeting moieties can be achieved through bioconjugation chemistries to impart new Functionalities. Various polymeric nanoparticles have been used for the formulation of nanoparticles such as naturally-occurring protein cages, virus-like particles, polymeric saccharides, and liposomes. These polymers have been proven to be biocompatible, side effects free and degradable with no toxicity. Objectives:: This paper reviews available literature on the nanoparticles pharmaceutical and medical applications. The review highlights and updates the customized solutions for selective drug delivery systems that allow high-affinity binding between nanoparticles and the target receptors. Methods:: Bibliographic databases and web-search engines were used to retrieve studies that assessed the usability of nanoparticles in the pharmaceutical and medical fields. Data were extracted on each system in vivo and in vitro applications, its advantages and disadvantages, and its ability to be chemically and genetically modified to impart new functionalities. Finally, a comparison between naturally occurring and their synthetic counterparts was carried out. Results:: The results showed that nanoparticles-based systems could have promising applications in diagnostics, cell labeling, contrast agents (Magnetic Resonance Imaging and Computed Tomography), antimicrobial agents, and as drug delivery systems. However, precautions should be taken to avoid or minimize toxic effect or incompatibility of nanoparticles-based systems with the biological systems in case of pharmaceutical or medical applications. Conclusion:: This review presented a summary of recent developments in the field of pharmaceutical nanotechnology and highlighted the challenges and the merits that some of the nanoparticles- based systems both in vivo and in vitro systems.

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Drug Delivery Systems For Anti-Cancer Active Complexes of Some Coinage Metals

Current Medicinal Chemistry ◽

10.2174/0929867324666170511152441 ◽

2018 ◽

Vol 25 (4) ◽

pp. 493-505 ◽

Cited By ~ 7

Author(s):

Ming Zhang ◽

Camille Saint-Germain ◽

Guiling He ◽

Raymond Wai-Yin Sun

Keyword(s):

Drug Delivery ◽

Metal Complexes ◽

Drug Delivery Systems ◽

Platinum Complexes ◽

Delivery Systems ◽

Development Of Resistance ◽

Anti Cancer ◽

Coinage Metals

Background: Although cisplatin and a number of platinum complexes have widely been used for the treatment of neoplasia, patients receiving these treatments have frequently suffered from their severe toxic side effects, the development of resistance with consequent relapse. In the recent decades, numerous complexes of coinage metals including that of gold, copper and silver have been reported to display promising in vitro and/or in vivo anti-cancer activities as well as potent activities towards cisplatin-resistant tumors. Nevertheless, the medical development of these metal complexes has been hampered by their instability in aqueous solutions and the nonspecific binding in biological systems. Methods: One of the approaches to overcome these problems is to design and develop adequate drug delivery systems (DDSs) for the transport of these complexes. By functionalization, encapsulation or formulation of the metal complexes, several types of DDSs have been reported to improve the desired pharmacological profile of the metal complexes, improving their overall stability, bioavailability, anti-cancer activity and reducing their toxicity towards normal cells. Conclusion: In this review, we summarized the recent findings for different DDSs for various anti- cancer active complexes of some coinage metals.

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Evaluation of Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) for Poorly Water-Soluble Talinolol: Preparation, in vitro and in vivo Assessment

Frontiers in Pharmacology ◽

10.3389/fphar.2019.00459 ◽

2019 ◽

Vol 10 ◽

Cited By ~ 21

Author(s):

Mohsin Kazi ◽

Mohammed Al-Swairi ◽

Ajaz Ahmad ◽

Mohammad Raish ◽

Fars K. Alanazi ◽

...

Keyword(s):

Drug Delivery ◽

Drug Delivery Systems ◽

Delivery Systems ◽

Water Soluble ◽

Poorly Water Soluble ◽

In Vivo Assessment

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Development of Self-Microemulsifying Drug Delivery Systems of Poorly Water-Soluble Pazopanib for Improvement of Oral Absorption

Science of Advanced Materials ◽

10.1166/sam.2020.3649 ◽

2020 ◽

Vol 12 (1) ◽

pp. 152-160

Author(s):

Sung-Up Choi ◽

Mi Jeong Kim ◽

Sung Tae Kim ◽

Hee-Cheol Kim ◽

Kwan Hyung Cho ◽

...

Keyword(s):

Drug Delivery ◽

Oral Delivery ◽

Drug Delivery Systems ◽

Oral Absorption ◽

Delivery Systems ◽

Water Soluble ◽

Pharmacokinetic Parameters ◽

Poorly Water Soluble

Self-microemulsifying drug delivery systems represent a stable formulation for enhancing the solubility and absorption efficacy of poorly soluble drugs. In this study, a self-microemulsifying drug delivery system (SMEDDS) was designed and applied for oral administration of poorly water-soluble pazopanib, a Biopharmaceutical Classification Class II anticancer drug. The solubility of pazopanib was first evaluated using various oils, surfactants, and co-surfactants. Pseudoternary phase diagrams were plotted to identify the selfemulsifying region and the phase behavior of optimized vehicle selected after screening of oils, surfactants, and co-surfactants. The SMEDDS comprising Capmul MCM NF, Tween 80, and PEG 400 was fabricated for incorporating pazopanib. It exhibited spherical droplets with size of 86.9 ± 0.8 nm and zeta potential value of –14.7 ± 0.1 mV. In vitro dissolution profiles of the SMEDDS were 2.40-fold (pH 4.0) and 6.45-fold (pH 6.8) higher than that of pazopanib powder. In particular, pazopanib-SMEDDS showed pH-independent dissolution profiles. In vivo pharmacokinetic parameters of the SMEDDS revealed enhanced bioavailability of pazopanib, which was 3.32-fold higher than that of pazopanib powder when administered orally. Taken together, the SMEDDS is effective as an oral delivery vehicle for pazopanib. In addition, our findings demonstrate that self-microemulsifying drug delivery systems could be a potential tool for improving bioavailability of other poorly water-soluble drugs.

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NANO/MICROSCALE TECHNOLOGIES FOR DRUG DELIVERY

Journal of Mechanics in Medicine and Biology ◽

10.1142/s021951941100406x ◽

2011 ◽

Vol 11 (02) ◽

pp. 337-367 ◽

Cited By ~ 7

Author(s):

HAIRUI LI ◽

JASPREET SINGH KOCHHAR ◽

JING PAN ◽

SUI YUNG CHAN ◽

LIFENG KANG

Keyword(s):

Drug Delivery ◽

Drug Delivery Systems ◽

Drug Testing ◽

New Technologies ◽

Delivery Systems ◽

In Vitro Tests ◽

In Vivo Test ◽

Micro Particles

Nano- and microscale technologies have made a marked impact on the development of drug delivery systems. The loading efficiency and particle size of nano/micro particles can be better controlled with these new technologies than conventional methods. Moreover, drug delivery systems are moving from simple particles to smart particles and devices with programmable functions. These technologies are also contributing to in vitro and in vivo drug testing, which are important to evaluate drug delivery systems. For in vitro tests, lab-on-a-chip models are potentially useful as alternatives to animal models. For in vivo test, nano/micro-biosensors are developed for testing chemicals and biologics with high sensitivity and selectivity. Here, we review the recent development of nanoscale and microscale technologies in drug delivery including drug delivery systems, in vitro and in vivo tests.

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Mechanisms and Pharmaceutical Action of Lipid Nanoformulation of Natural Bioactive Compounds as Efficient Delivery Systems in the Therapy of Osteoarthritis

Pharmaceutics ◽

10.3390/pharmaceutics13081108 ◽

2021 ◽

Vol 13 (8) ◽

pp. 1108

Author(s):

Oana Craciunescu ◽

Madalina Icriverzi ◽

Paula Ecaterina Florian ◽

Anca Roseanu ◽

Mihaela Trif

Keyword(s):

Drug Delivery ◽

Bioactive Compounds ◽

Targeted Delivery ◽

Drug Delivery Systems ◽

Delivery Systems ◽

Joint Disease ◽

Duration Of Action ◽

Immune System Activation

Osteoarthritis (OA) is a degenerative joint disease. An objective of the nanomedicine and drug delivery systems field is to design suitable pharmaceutical nanocarriers with controllable properties for drug delivery and site-specific targeting, in order to achieve greater efficacy and minimal toxicity, compared to the conventional drugs. The aim of this review is to present recent data on natural bioactive compounds with anti-inflammatory properties and efficacy in the treatment of OA, their formulation in lipid nanostructured carriers, mainly liposomes, as controlled release systems and the possibility to be intra-articularly (IA) administered. The literature regarding glycosaminoglycans, proteins, polyphenols and their ability to modify the cell response and mechanisms of action in different models of inflammation are reviewed. The advantages and limits of using lipid nanoformulations as drug delivery systems in OA treatment and the suitable route of administration are also discussed. Liposomes containing glycosaminoglycans presented good biocompatibility, lack of immune system activation, targeted delivery of bioactive compounds to the site of action, protection and efficiency of the encapsulated material, and prolonged duration of action, being highly recommended as controlled delivery systems in OA therapy through IA administration. Lipid nanoformulations of polyphenols were tested both in vivo and in vitro models that mimic OA conditions after IA or other routes of administration, recommending their clinical application.

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