Chitosan as Valuable Excipient for Oral and Topical Carvedilol Delivery Systems

Chitosan is a valued excipient due to its biocompatibility properties and increasing solubility of poorly water-soluble drugs. The research presented in this paper concerns the preparation of binary combinations of chitosan (deacetylated chitin) with carvedilol (beta-blocker) to develop a formulation with a modified carvedilol release profile. As part of the research, six physical mixtures of chitosan with carvedilol were obtained and identified by spectral (PXRD, FT-IR, and Raman), thermal (DSC), and microscopic (SEM) methods. The next stage of the research estimated the profile changes and the dissolution rate for carvedilol in the obtained drug delivery systems; the reference sample was pure carvedilol. The studies were conducted at pH = 1.2 and 6.8, simulating the gastrointestinal tract conditions. Quantitative changes of carvedilol were determined using the developed isocratic UHPLC-DAD method. Established apparent permeability coefficients proved the changes in carvedilol’s permeability after introducing a drug delivery system through membranes simulating the gastrointestinal tract and skin walls. A bioadhesive potential of carvedilol–chitosan systems was confirmed using the in vitro model. The conducted research and the obtained results indicate a significant potential of using chitosan as an excipient in modern oral or epidermal drug delivery systems of carvedilol.

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Rationalizing the selection of oral lipid based drug delivery systems by an in vitro dynamic lipolysis model for improved oral bioavailability of poorly water soluble drugs

Journal of Controlled Release ◽

10.1016/j.jconrel.2008.03.021 ◽

2008 ◽

Vol 129 (1) ◽

pp. 1-10 ◽

Cited By ~ 198

Author(s):

Arik Dahan ◽

Amnon Hoffman

Keyword(s):

Drug Delivery ◽

Oral Bioavailability ◽

Drug Delivery Systems ◽

Delivery Systems ◽

Water Soluble ◽

Poorly Water Soluble Drugs ◽

Water Soluble Drugs ◽

Poorly Water Soluble ◽

Selection Of

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Innovative Strategies for Lipid-Based Drug Delivery

Multifunctional Nanocarriers for Contemporary Healthcare Applications - Advances in Medical Technologies and Clinical Practice ◽

10.4018/978-1-5225-4781-5.ch004 ◽

2018 ◽

pp. 60-84 ◽

Cited By ~ 1

Author(s):

Navneet Sharma ◽

Sabna Kotta ◽

Mohd Aleem ◽

Shubham Singh ◽

Rakesh Kumar Sharma

Keyword(s):

Drug Delivery ◽

Drug Absorption ◽

Drug Delivery Systems ◽

Delivery Systems ◽

Water Soluble ◽

Absorption Process ◽

Innovative Strategies ◽

The Poor ◽

Water Soluble Drugs ◽

Selection Of

In the last decade, there has been a mounting concern in lipid-based formulations to deliver water-soluble drugs. Lipid-based drug delivery systems are one of the budding and promising technologies designed to tackle the poor bioavailability problems. This chapter stresses the different mechanisms of lipophilic drug absorption along with its advantages and limitations. It points out the different mechanisms of how lipid-based excipients and the different formulations interact with the absorption process. This review provides a comprehensive summary about the lipid formulation classification scheme (LFCS), a guide for the selection of appropriate formulation and commonly used excipients for lipid-based formulations, along with the important factors to be considered in formulation design and excipient selection. This review also focuses on the formulation of solid lipid-based formulations, important evaluation aspects, and commercial formulations available for the purpose.

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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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Lipid-based systems as a promising approach for enhancing the bioavailability of poorly water-soluble drugs

Acta Pharmaceutica ◽

10.2478/acph-2013-0040 ◽

2013 ◽

Vol 63 (4) ◽

pp. 427-445 ◽

Cited By ~ 70

Author(s):

Katja Čerpnjak ◽

Alenka Zvonar ◽

Mirjana Gašperlin ◽

Franc Vrečer

Keyword(s):

Drug Delivery ◽

Oral Bioavailability ◽

Drug Delivery Systems ◽

Water Solubility ◽

Pharmaceutical Products ◽

Delivery Systems ◽

Water Soluble ◽

Poorly Water Soluble Drugs ◽

Water Soluble Drugs ◽

Poorly Water Soluble

Abstract Low oral bioavailability as a consequence of low water solubility of drugs is a growing challenge to the development of new pharmaceutical products. One of the most popular approaches of oral bioavailability and solubility enhancement is the utilization of lipid-based drug delivery systems. Their use in product development is growing due to the versatility of pharmaceutical lipid excipients and drug formulations, and their compatibility with liquid, semi-solid, and solid dosage forms. Lipid formulations, such as self-emulsifying (SEDDS), self-microemulsifying SMEDDS) and self- -nanoemulsifying drug delivery systems (SNEDDS) were explored in many studies as an efficient approach for improving the bioavailability and dissolution rate of poorly water-soluble drugs. One of the greatest advantages of incorporating poorly soluble drugs into such formulations is their spontaneous emulsification and formation of an emulsion, microemulsion or nanoemulsion in aqueous media. This review article focuses on the following topics. First, it presents a classification overview of lipid-based drug delivery systems and mechanisms involved in improving the solubility and bioavailability of poorly water-soluble drugs. Second, the article reviews components of lipid-based drug delivery systems for oral use with their characteristics. Third, it brings a detailed description of SEDDS, SMEDDS and SNEDDS, which are very often misused in literature, with special emphasis on the comparison between microemulsions and nanoemulsions.

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A Comprehensive Review on Self-Nano Emulsifying Drug Delivery Systems: Advancements & Applications

International Journal of Pharmaceutical Sciences and Drug Research ◽

10.25004/ijpsdr.2020.120522 ◽

2020 ◽

pp. 576-583

Author(s):

Srikanth Reddy Sokkula ◽

Suresh Gande

Keyword(s):

Drug Delivery ◽

Drug Delivery Systems ◽

Large Scale ◽

Antihypertensive Drugs ◽

Drug Loading ◽

Delivery Systems ◽

Water Soluble ◽

Scale Production ◽

Advantages And Disadvantages ◽

Water Soluble Drugs

Lipid-based drug delivery systems are extensively reported in literature for enhancing the drug solubility, permeability and bioavailability. These systems include simple oil solutions, coarse, multiple and dry emulsions, complex self-emulsifying, microemulsifying or nanoemulsifying drug delivery systems. Self-emulsifying systems are further classified as self-microemulsifying drug delivery systems (SMEDDS) and self-nanoemulsifying drug delivery systems (SNEDDS) are most prevailing and commercially viable oil based approach for drugs that exhibit low dissolution rate and inadequate absorption. Ever since the progress of SNEDDS, they drew the interest of researchers in order to deal with the challenges of poorly water-soluble drugs. SNEDDS is a proven method for enhancing solubility and bioavailability of lipophilic compounds. Considering the ease of large-scale production and the robustness of SNEDDS, several formulations techniques are commercially available. The stability of SNEDDS can be further enhanced by solidifying liquid SNEDDS. Controlled release and supersaturated SNEDDS received patient compliance with larger drug loading. Presence of biodegradable ingredients and ‘drug-targeting opportunities’ facilitate SNEDDS a clear merit and distinction amongst available solubility enhancement techniques. In this article attempt was made to present an overview of SNEDDS, their mechanism, formulation excipients and potentials of SNEDDS, recent advancements, advantages and disadvantages of SNEDDS formulations. The article also focuses on reviewing the application of SNEDDS in enhancing bioavailability of antihypertensive drugs.

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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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Successful oral delivery of poorly water-soluble drugs both depends on the intraluminal behavior of drugs and of appropriate advanced drug delivery systems

European Journal of Pharmaceutical Sciences ◽

10.1016/j.ejps.2019.104967 ◽

2019 ◽

Vol 137 ◽

pp. 104967 ◽

Cited By ~ 52

Author(s):

Ben J. Boyd ◽

Christel A.S. Bergström ◽

Zahari Vinarov ◽

Martin Kuentz ◽

Joachim Brouwers ◽

...

Keyword(s):

Drug Delivery ◽

Oral Delivery ◽

Drug Delivery Systems ◽

Delivery Systems ◽

Water Soluble ◽

Poorly Water Soluble Drugs ◽

Water Soluble Drugs ◽

Poorly Water Soluble

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FORMULATION, DEVELOPMENT AND CHARACTERIZATION OF DRUG DELIVERY SYSTEMS BASED TELMISARTAN ENCAPSULATED IN SILK FIBROIN NANOSPHERE’S

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2019v11i1.30588 ◽

2019 ◽

Vol 11 (1) ◽

pp. 247 ◽

Cited By ~ 1

Author(s):

Shahid Ud Din Wani ◽

Gangadharappa H. V. ◽

Ashish N. P.

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Zeta Potential ◽

Silk Fibroin ◽

Drug Delivery Systems ◽

Delivery Systems ◽

Water Soluble ◽

Random Coil ◽

Burst Release

Objective: The aim of the present work was to formulate silk fibroin (SF) nanospheres (NS’s) for drug delivery application. The current study was designed to advance the water solubility and bio-availability of telmisartan by nanoprecipitation method.Methods: SF NS’s loaded with TS were prepared by nanoprecipitation method. The drug was dissolved in aqueous solution of SF by using acetone as a non-solvent. The prepared NS’s were then characterized by FTIR, X-ray diffraction and zeta potential, and were evaluated for its, surface morphology, %drug content, encapsulation efficiency and in vitro drug release.Results: The evaluation results of SF NS’s loaded of TS showed 74.22±0.17 % entrapment efficiency, 35.21±0.02 % of drug loading, and-4.9 mV to-13.6 mV of zeta potential due to the proper bounding of TS with the β-sheets of SF, the particle size reported was within the size range of 160-186 nm having smooth surface and were spherical in shape. The SFNS’s pattern switched from random coil to β-sheet formation on treating with acetone. FTIR and DSC studies marked no such inter-molecular interactions between SF and drug molecules. The % cumulative in vitro drug release from SF NS’s exhibited quick burst release. The in vitro cumulative drug release of SF NS’s of TS it was found that about 74% of the drug was released within 8 h and about 96% of drug released at 24 hr. The rate of drug release increased with the increase in SF ratio.Conclusion: It is believed that these SF NS’s will find potential applications in drug delivery release as drug carriers, especially poor water-soluble drugs. All these results proposed that SF NS’s are eventuality handy in various drug delivery systems.

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