A Conceptual Analysis of solid Self-emulsifying drug Delivery System and its Associate Patents for the Treatment of Cancer

Author(s):  
Neeraj Singh ◽  
Shweta Rai ◽  
Sankha Bhattacharya

Background: About two-third of new drugs reveal low solubility in water due to that; it becomes difficult for formulation scientists to develop oral solid dosage forms with a pharmaceutically acceptable range of therapeutic activity. In such cases, S-SMEEDS are the best carrier used universally for the delivery of hydrophobic drugs. SEDDS were also used, but due to its limitations, S-SMEDDS used widely. These are the isotropic mixtures of oils, co-solvents, and surfactants. S-SMEDDS are physically stable, easy to manufacture, easy to fill in gelatin capsules as well as improves the drug bioavailability by releasing the drug in the emulsion form to the gastrointestinal tract and make smooth absorption of the drug through the intestinal lymphatic pathway. Methods: We took on the various literature search related to our review, including the peer-reviewed research, and provided a conceptual framework to that. Standard tools are used for making the figures of the paper, and various search engines are used for the literature exploration.In this review article the author discussed the importance of S-SMEDDS, selection criteria for excipients, pseudo-ternary diagram, mechanism of action of S-SMEDDS, solidification techniques used for S-SMEDDS, Characterization of SEDDS and S-SMEDDS including Stability Evaluation of both and future prospect concluded through recent findings on S-SMEDDS on Cancer as well as a neoteric patent on S-SMEDDS Results: Many research papers discussed in this review article, from which it was found that the ternary phase diagram is the most crucial part of developing the SMEDDS. From the various research findings, it was found that the excipient selection is the essential step which decides the strong therapeutic effect of the formulation. The significant outcome related to solid-SMEDDS is less the globule size, higher would be the bioavailability. The adsorption of a solid carrier method is the most widely used method for the preparation of solid-SMEDDS. After review of many patents, it is observed that the solid-SMEDDS have a strong potential for targeting and treatment of a different type of Cancer due to their property to enhance permeation and increased bioavailability. Conclusion: S-SMEEDS are more acceptable pharmaceutically as compare to SEDDS due to various advantages over SEDDS viz stability issue is prevalent with SEDDS. A number of researchers had formulated S-SMEDDS of poorly soluble drugs and founded S-SMEDDS as prospective for the delivery of hydrophobic drugs for the treatment of Cancer. S-SMEEDS are grabbing attention, and the patentability on S-SMEDDS is unavoidable, these prove that S-SMEEDS are widely accepted carriers. These are used universally for the delivery of the hydrophilic drugs and anticancer drugs as it releases the drug to the gastrointestinal tract and enhances the systemic absorption. Abstract: Majority of active pharmaceutical ingredients (API) shows poor aqueous solubility, due to that drug delivery of the API to the systemic circulation becomes difficult as it has low bioavailability. The bioavailability of the hydrophobic drugs can be improved by the Self-emulsifying drug delivery system (SEDDS) but due to its various limitations, solid self-micro emulsifying drug delivery systems (S-SMEDDS) are used due to its advantages over SEDDS. S-SMEDDS plays a vital role in improving the low bioavailability of poorly aqueous soluble drugs. Hydrophobic drugs can be easily loaded in these systems and release the drug to the gastrointestinal tract in the form of fine emulsion results to In-situ solubilisation of the drug. In this review article the author's gives an overview of the solid SMEDSS along with the solidification techniques and an update on recent research and patents filled for Solid SMEDDS.

2021 ◽  
Vol 2071 (1) ◽  
pp. 012026
Author(s):  
A M Noor ◽  
Z Zakaria ◽  
S Johari ◽  
N Sabani ◽  
Y Wahab ◽  
...  

Abstract Transdermal Iontophoretic Drug Delivery System (TIDDS) is a non-invasive method of systemic drug delivery that involves by applying a drug formulation to the skin. The drug penetrates through the stratum corneum, epidermis and dermis layers. Once the drug reaches the dermal layer, it is available for systemic absorption via dermal microcirculation. However, clinical testing of new drug developed for the iontophoretic system is a long and complex process. Recently, most of those major pharmaceutical companies have attempted to consider computer-based bio-simulation strategies as a means of generating the data necessary to help make a better decision. In this work, we used computational modelling to investigate the TIDDS behaviour. Our interest is to study the efficacy of drug diffusion through transdermal delivery, including the thermal effect on the skin. We found that drug will be delivered more efficiently if the electrical potential and the position of electrodes are optimum. We analysed the drug diffusion time of the system using 1,3 and 5 mA DC source. In addition, we also modify the electrode distance from 10 mm to 30 mm long and analysed the effect of delivery time and d effect to the skin thermal. We conclude that, a high electrical current, as instance, a 5 mA DC, delivered the drug faster into the skin but increased the skin temperature because of skin joule heating effect. However, a 30 mm electrodes distance setting decreased the skin temperature significantly than the 10 mm distance with more than 9.7 °C under 5 mA DC and 60 minutes of operation. TIDDS enhanced drug delivery compared to oral consumption and might be suitable used for localizing treatments such as chronic disease. This work provides great potential and is useful to efficiently design of iontophoretic drug delivery system including new drugs delivery applications.


Author(s):  
Dinesh Kaushik ◽  
Jyoti Malik ◽  
Satish Sardana ◽  
Chisa Matsubara

Oral route is the most preferred route of drug administration due to its easy accessibility, intake, and wide range of choices making it economical. Currently, greater than 60% of marketed drugs are oral products. Over 90% of therapeutic compounds given orally areknown to possess oral bioavailability limitations. Therefore, there is a need to explore various approaches that can be used to improve oral drug bioavailability besides using physical and chemical means. The objective of this study is to prepare a formulation i.e. self microemulsifying drug delivery system (SMEDDS) of nifedipine with the intention to improve the increase dissolution rate (solubility). This will ensure the quick absorption and uniform bioavailability of nifedipine. Selection of oils, surfactants and co-surfactants was done by determining % transparency and on the basis of compatibility studies by FTIR spectra analysis. Different SMEDDS formulation were prepared of different ratio of oil:surfactantmix (1:9,2:8,3:7,4:6,5:5,6:4,7:3,8:2,9:1) and different ratio of surfactants : cosurfactants. Pseudo ternary phase diagram were constructed by water titration method to obtain a particle micro-emulsion region (on the basis of clarity and transparency). The formulation B-I was optimized because of maximum transparency (87.35%) and maximum % drug entrapment (95.32%). The average droplet size and zeta potential was found 86.05 and -0.189. The solubility of nifedipine increase in SMEDDS formulation upto72.17%.From in vitro dissolution study it was proved that SMEDDS formulation releases drug at faster rate, thus the objective of increase solubility and hence the better dissolution rate for uniform bioavailability via SMEDDS formulation of nifedipine was successfully achieved.


Author(s):  
Vikrant P Wankhade ◽  
Nivedita S Kale ◽  
K.K Tapar

Many chemical entities and nutraceuticals are poor water soluble and show high lipophilicity. It’s difficult to formulate them into oral formulation because of its low aqueous solubility which ultimately affects bioavailability. To enhance the bioavailability of such drugs compounds, self microemulsifying drug delivery system is the reliable drug delivery system. In this system the drug is incorporated in the isotropic system and formulated as unit dosage form. Self microemulsifying drug delivery system is the novel emulsified system composed of anhydrous isotropic mixture of oils, surfactant, and co solvent and sometimes co surfactant. Drug is directly dispersed into the entire gastro intestinal tract with continuous peristaltic movement and drug is available in the solution form of microemulsion, absorbed through lymphatic system and bypasses the dissolution step. Hence they increase the patient compliance. The excipients are selected on basis of construction of ternary phase diagram. Self micro-emulsifying drug delivery system is very useful for drug in which drug dissolution is rate limiting step. This review describes the novel approaches and evaluation parameters of the self microemulsifying drug delivery system towards different classic drugs, proteins-peptides, and nutraceuticals in various oral microemulsion compositions and microstructures.


Author(s):  
Kanuri Lakshmi Prasad ◽  
Kuralla Hari

Objective: To enhance solubility and dissolution rate of budesonide through development of solid self-nanoemulsifying drug delivery system (S-SNEDDS). Methods: Liquid self-nanoemulsifying drug delivery systems (L-SNEDDS) were prepared and ternary phase diagram was constructed using Origin pro 8. Liquid self-nanoemulsifying formulation LF2 having 20% oil and 80% of surfactant/co-surfactant was optimized from the three formulations (LF1-LF3) to convert in to solid, through various characterization techniques like self-emulsification, in vitro drug release profile and drug content estimation. The prepared L-SNEDDS converted into S-SNEDDS, SF1-SF6 by adsorption technique using Aerosil 200, Neusilin US2, and Neusilin UFL2 to improve flowability, compressibility and stability. Results: Formulation LF2 exhibited globule size of 82.4 nm, PDI 0.349 and Zeta potential -28.6 mV with drug indicating the stability and homogeneity of particles. The optimized formulation SF4 containing Neusilin UFL2 was characterized by DSC, FTIR, X-Ray diffraction studies and found no incompatibility and no major shifts were noticed. Formulation SF4 released 100 % drug in 20 min against pure drug release of 47 % in 60 min. Regardless of the form (i.e. liquid or solid) similar performance of emulsification efficiency is observed. Conclusion: The results demonstrated that the technique of novel solid self-nanoemulsifying drug delivery system can be employed to enhance the solubility and dissolution rate of poorly water-soluble drug budesonide.


Author(s):  
Swapnil S. Bornare ◽  
Smita S. Aher ◽  
Ravindranath B. Saudagar

Film forming gels are a novel approach in this area that might present an alternative to the conventional dosage forms used on the skin, such as ointments, creams, gels or patches. The polymeric solution is applied to the skin as a liquid and forms an almost invisible film in situ by solvent evaporation. Transdermal drug delivery system (TDDS) and dermal drug delivery system can provide some desirable performances over conventional pharmaceutical dosage formulations, such as avoiding gut and hepatic first-pass metabolism, improving drug bioavailability, reducing dose frequency and stabilizing drug delivery profiles. The aim of this review was to search for alternatives to the conventional forms in order to reduce skin irritation, improve skin adhesion properties, enhance the drug release and increase the patient acceptability from an aesthetic perspective. Because of their peculiar rheological behaviour, polymeric gels are beneficial in terms of ease of preparation, ease of application, adhesion to the application surface and ability to deliver a wide variety of drugs.


Author(s):  
Anupam K Sachan ◽  
Saurabh Singh ◽  
Kiran Kumari ◽  
Pratibha Devi

Microspheres carrier system made from natural or synthetic polymers used in sustained release drug delivery system. The present study involves formulation and evaluation of floating microspheres of Curcumin for improving the drug bioavailability by prolongation gastric residence time. Curcumin, natural hypoglycemic agent is a lipophilic drug, absorbed poorly from the stomach, quickly eliminated and having short half-life so suitable to formulate floating drug delivery system for sustained release. Floating microspheres of curcumin were formulated by solvent evaporation technique using ethanol and dichloromethane (1:1) as organic solvent and incorporating various synthetic polymers as coating polymer, sustain release polymers and floating agent. The final formulation were evaluated various parameters such as compatibility studies, micrometric properties, In-vitro drug release and % buoyancy. FTIR studies showed that there were no interaction between drug and excipients. The surface morphology studies by SEM confirmed their spherical and smooth surface. The mean particles size were found to be 416-618µm, practical yield of microspheres was in the range of 60.21±0.052% - 80.87±0.043%, drug entrapment efficiency 47.4±0.065% - 77.9±0.036% and % buoyancy 62,24±0.161% - 88.63±0.413%. Result show that entraptmency increased as polymer (Eudragit RS100) conc. Increased. The drug release after 12 hrs. was 72.13% - 87.13% and it decrease as a polymer (HPMC, EC) concentration was decrease.


2019 ◽  
Vol 7 (4) ◽  
pp. 328-338
Author(s):  
Rajan Kalamkar ◽  
Shailesh Wadher

Background: Phosal based excipients are liquid concentrates containing phospholipids. They are used to solubilize water-insoluble drug and also act as an emulsifier to get the smallest droplet size of the formed emulsion after administration. Objective: The aim is to prepare phosal based self nanoemulsifying drug delivery system (SNEDDS) for water insoluble drug zaltoprofen. Methods: The various parameters like solubility of drug in different vehicles, ternary phase diagram are considered to formulate the stable emulsion which is further characterized by Self emulsification time and globule size analysis to optimize liquid SNEDDS of Zaltoprofen. Optimized L-SNEDDS was converted into free-flowing powder Solid-SNEDDS (S-SNEDDS). S-SNEDDS was evaluated for Globule size analysis after reconstitution, in vitro dissolution study and in vivo pharmacokinetic study in rats. Results: Phosal 53 MCT with highest drug solubility was used as oil along with Tween 80 and PEG 400 as surfactant and cosurfactant respectively to prepare liquid SNEDDS. Neusilin us2 was used as an adsorbent to get free-flowing S-SNEDDS. S-SNEDDS showed improved dissolution profile of the drug as compared to pure drug. In vivo study demonstrated that there is a significant increase in Cmax and AUC of S-SNEDDS compared to zaltoprofen powder. Conclusion: Phosal based SNEDDS formation can be successfully used to improve the dissolution and oral bioavailability of poorly soluble drug zaltoprofen.


Author(s):  
Vibhavari M. Chatur ◽  
Shashikant N. Dhole

Infectious disease treatment and immunisation have undergone a transformative change in recent years. With the advancement of biotechnology and genetic engineering, a large number of disease-specific biological have been created, as well as a focus on delivering these biological effectively. Niosomes are vesicular Nano carriers that are gaining popularity as a potential transdermal drug delivery system due to properties like enhanced drug penetration, a local depot for sustained drug release, and a rate-limiting membrane for modulating systemic absorption of drugs through the skin. Niosomes are non-ionic surfactant-based vesicles that are biodegradable, relatively nontoxic, more stable, and less expensive than liposomes. This analysis gives a high-level overview of niosomes, including their chemical composition, structure, benefits, and applications, as well as some general observations on niosomes as percutaneous permeation enhancers.


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