A Review on Recent Controlled Release Strategies for Oral Drug Delivery of Repaglinide (a BCS Class II Drug)

2021 ◽  
Vol 10 ◽  
Author(s):  
Saba Albetawi ◽  
Amer Abdalhafez ◽  
Ala Abu-Zaid
Keyword(s):  
Drug Delivery ◽  
Oral Delivery ◽  
Pancreatic Beta Cells ◽  
Water Solubility ◽  
Oral Drug Delivery ◽  
Aqueous Solubility ◽  
Class Ii ◽  
Oral Drug ◽  
Log P ◽  
P Value

: Repaglinide is an antidiabetic drug that works by stimulating insulin secretion from pancreatic beta cells. Repaglinide is practically insoluble in water with a water solubility of 34 µg/mL at 37 ˚C, and it has a high absorption rate from the gastrointestinal tract following oral administration since the log P value of repaglinide is 3.97. The low aqueous solubility and the high permeability of repaglinide represent a typical behavior for drugs that belong to class II Biopharmaceutical Classification System (BCS II). Managing type-2 diabetes mellitus with repaglinide is considered a burdensome therapy, as it requires frequent dosing of repaglinide before each meal to maintain its therapeutic plasma concentration due to its short plasma half-life of approximately one hour. Hence the present review aims to discuss thoroughly the various approaches investigated in recent years to develop drug delivery systems that improve oral delivery of repaglinide, including nanoemulsions, solid lipid nanoparticles, nanostructured lipid carriers, sustained-release hydrophilic matrix, floating microspheres, and nanocomposites.

scholarly journals Self-Nano-Emulsifying Drug-Delivery Systems: From the Development to the Current Applications and Challenges in Oral Drug Delivery

Pharmaceutics ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 1194
Author(s):  
Aristote B. Buya ◽  
Ana Beloqui ◽  
Patrick B. Memvanga ◽  
Véronique Préat
Keyword(s):  
Drug Delivery ◽  
Patient Compliance ◽  
Oral Delivery ◽  
Drug Delivery Systems ◽  
Water Solubility ◽  
Oral Drug Delivery ◽  
Delivery Systems ◽  
Oral Drug ◽  
Statistical Design Of Experiments

Approximately one third of newly discovered drug molecules show insufficient water solubility and therefore low oral bio-availability. Self-nano-emulsifying drug-delivery systems (SNEDDSs) are one of the emerging strategies developed to tackle the issues associated with their oral delivery. SNEDDSs are composed of an oil phase, surfactant, and cosurfactant or cosolvent. SNEDDSs characteristics, their ability to dissolve a drug, and in vivo considerations are determinant factors in the choice of SNEDDSs excipients. A SNEDDS formulation can be optimized through phase diagram approach or statistical design of experiments. The characterization of SNEDDSs includes multiple orthogonal methods required to fully control SNEDDS manufacture, stability, and biological fate. Encapsulating a drug in SNEDDSs can lead to increased solubilization, stability in the gastro-intestinal tract, and absorption, resulting in enhanced bio-availability. The transformation of liquid SNEDDSs into solid dosage forms has been shown to increase the stability and patient compliance. Supersaturated, mucus-permeating, and targeted SNEDDSs can be developed to increase efficacy and patient compliance. Self-emulsification approach has been successful in oral drug delivery. The present review gives an insight of SNEDDSs for the oral administration of both lipophilic and hydrophilic compounds from the experimental bench to marketed products.

Self-micro Emulsifying Drug Delivery System “SMEDDS” for Efficient Oral Delivery of Andrographolide

2020 ◽  
Vol 10 (1) ◽  
pp. 38-53 ◽  
Author(s):  
Sivaram Nallamolu ◽  
Vijaya R. Jayanti ◽  
Mallikarjun Chitneni ◽  
Liew Y. Khoon ◽  
Prashant Kesharwani
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
Water Solubility ◽  
Oral Drug Delivery ◽  
Drug Loading ◽  
Oral Drug ◽  
Breast Cancer Cell Lines ◽  
Dissolution Profile

Objective: Andrographolide has potent anticancer and antimicrobial activity; however, its clinical application has been limited due to its poor water solubility as well as lack of appropriate formulation. The objective of this investigation was to formulate Self–Micro Emulsifying Drug Delivery System (SMEDDS) of andrographolide and explore its oral drug delivery aptitudes. Methods: Andrographolide SMEDDS was optimized by ternary phase approach and studied for various in vitro characteristics: Particle size, electron microscopy, polydispersity index, surface charge, dilution effect, pH stability, freeze-thaw effect, dissolution profile and stability studies. Further, antimicrobial and cytotoxic performance of andrographolide SMEDDS were evaluated in MCF–7 breast cancer cell lines and methicillin-resistant microorganisms, respectively. Results: An optimized SMEDDS formulation of andrographolide was successfully prepared and evaluated for its drug delivery potential. The solubility of andrographolide in the developed SMEDDS formulation was increased significantly, and the drug loading was enough for making this drug clinically applicable. The andrographolide SMEDDS formulation competitively inhibited the growth of microorganisms and showed enhanced anti–microbial activity against MRSA microorganisms. Conclusion: The SMEDDS strategy represents one of the best approaches to deliver andrographolide via oral route, while resolving its solubility limitations.

scholarly journals SELF-MICROEMULSIFYING DRUG DELIVERY SYSTEM

2016 ◽  
pp. 33
Author(s):  
Sonia Anand ◽  
Rishikesh Gupta ◽  
Prajapati Sk
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Water Solubility ◽  
Oral Absorption ◽  
Aqueous Solubility ◽  
Class Ii ◽  
Oral Route ◽  
Oral Drug ◽  
Liquid Form

<p>ABSTRACT<br />Oral route is the most convenient route of drug administration in many diseases and till today it is the first way investigated in the development of<br />new dosage forms. The major problem in oral drug formulations is low and erratic bioavailability, which mainly results from poor aqueous solubility,<br />thereby pretense problems in their formulation. More than 40% of potential drug products suffer from poor water solubility. For the therapeutic<br />delivery of lipophilic active moieties (biopharmaceutical classification system Class II drugs), lipid-based formulations are inviting increasing<br />attention. Currently, a number of technologies are available to deal with the poor solubility, dissolution rate, and bioavailability of insoluble drugs.<br />One of the promising techniques is self-microemulsifying drug delivery systems (SMEDDS). SMEDDS have gained exposure for their ability to increase<br />solubility and bioavailability of poorly soluble drugs. SMEDDS, which are isotropic mixtures of oils, surfactants, solvents, and co-solvents/surfactants<br />can be used for the design of formulations to improve the oral absorption of highly lipophilic drug compounds. Conventional SMEDDS are mostly<br />prepared in a liquid form, which can have some disadvantages. SMEDDS can be orally administered in soft or hard gelatin capsules and form fine<br />relatively stable oil-in-water emulsions. Solid-SMEDDS are prepared by solidification of liquid/semisolid self-micron emulsifying ingredients into<br />powders, have gained popularity. This article gives a complete overview of SMEDDS, but special attention has been paid to formulation, design,<br />evaluation, and little emphasis on application of SMEDDS.<br />Keywords: Self-microemulsifying drug delivery system, Surfactant, Oil, Co-surfactant, Bioavailability, Lipophilic, Biopharmaceutical classification<br />system Class II drugs.</p>

scholarly journals ORAL DRUG DELIVERY OF INSULIN IN DIABETES MELLITUS: AN ATTRACTIVE ALTERNATE TO OVERCOME INVASIVE ROUTE

2019 ◽  
Author(s):  
Pooja Mathur ◽  
Chandra Kant Mathur ◽  
Kanchan Mathur
Keyword(s):  
Diabetes Mellitus ◽  
Drug Delivery ◽  
Delivery System ◽  
Oral Delivery ◽  
Oral Drug Delivery ◽  
Relevant Information ◽  
Delivery Systems ◽  
Oral Drug ◽  
Oral Insulin ◽  
Human Beings

The subcutaneous injection of insulin for the treatment of diabetes mellitus can lead to patient non-compliance, discomfort, pain and local infection is a chronic metabolic health disease affecting the homeostasis of blood sugar levels in human beings. Oral route of drug delivery system has been the most widely accepted means of drug administration other than invasive drug delivery systems. For the development of an oral insulin delivery system, we have to focus on overcoming the various gastro-intestinal barriers for insulin uptake from the gastrointestinal tract. To overcome these barriers various types of formulations such as insulin conjugates, micro/nanoparticles, liposomes, hydrogel, capsule, and tablets are designed to deliver insulin orally. Various potential ways to administer insulin orally has been explored over years but a fluctuating level of insulin release have been recorded. A number of advancement has taken place in the recent years for understanding the needs of improved oral delivery systems of insulin. This review article concentrates on the challenges for oral drug delivery of insulin as well as various carriers used for the oral drug delivery of insulin and also provides the relevant information about the clinical tested formulations of oral insulin and its patents.

Nanoparticles with surface features of dendritic oligopeptides as potential oral drug delivery systems

2020 ◽  
Vol 8 (13) ◽  
pp. 2636-2649
Author(s):  
Yuli Bai ◽  
Rui Zhou ◽  
Lei Wu ◽  
Yaxian Zheng ◽  
Xi Liu ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Specific Surface ◽  
Oral Delivery ◽  
Drug Delivery Systems ◽  
Oral Drug Delivery ◽  
Delivery Systems ◽  
Oral Drug ◽  
Protein Drugs ◽  
Surface Features ◽  
Oral Drug Delivery Systems

Endowing the NPs with specific surface features of dendritic oligopeptides holds great potential for the oral delivery of peptide/protein drugs.

scholarly journals Nanotechnology-Based Biopolymeric Oral Delivery Platforms for Advanced Cancer Treatment

Cancers ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 522 ◽  
Author(s):  
Vanessa T. Chivere ◽  
Pierre P. D. Kondiah ◽  
Yahya E. Choonara ◽  
Viness Pillay
Keyword(s):  
Oral Delivery ◽  
Oral Drug Delivery ◽  
Specific Binding ◽  
Biological Effects ◽  
Aqueous Solubility ◽  
Oral Route ◽  
Oral Drug ◽  
Cancer Drugs ◽  
Anti Cancer ◽  
Route Of Delivery

Routes of drug administration and their corresponding physiochemical characteristics play major roles in drug therapeutic efficiency and biological effects. Each route of delivery has favourable aspects and limitations. The oral route of delivery is the most convenient, widely accepted and safe route. However, the oral route of chemotherapeutics to date have displayed high gastric degradation, low aqueous solubility, poor formulation stability and minimum intestinal absorption. Thus, mainstream anti-cancer drugs in current formulations are not suitable as oral chemotherapeutic formulations. The use of biopolymers such as chitosan, gelatin, hyaluronic acid and polyglutamic acid, for the synthesis of oral delivery platforms, have potential to help overcome problems associated with oral delivery of chemotherapeutics. Biopolymers have favourable stimuli-responsive properties, and thus can be used to improve oral bioavailability of anti-cancer drugs. These biopolymeric formulations can protect gastric-sensitive drugs from pH degradation, target specific binding sites for targeted absorption and consequently control drug release. In this review, the use of various biopolymers as oral drug delivery systems for chemotherapeutics will be discussed.

scholarly journals A Critical Appraisal of Solubility Enhancement Techniques of Polyphenols

2014 ◽  
Vol 2014 ◽  
pp. 1-14 ◽  
Author(s):  
Harkiran Kaur ◽  
Gurpreet Kaur
Keyword(s):  
Drug Delivery ◽  
Critical Appraisal ◽  
Oral Drug Delivery ◽  
Aqueous Solubility ◽  
Solubility Enhancement ◽  
Oral Drug ◽  
Natural Substances ◽  
First Pass ◽  
Cellular Dna

Polyphenols constitute a family of natural substances distributed widely in plant kingdom. These are produced as secondary metabolites by plants and so far 8000 representatives of this family have been identified. Recently, there is an increased interest in the polyphenols because of the evidence of their role in prevention of degenerative diseases such as neurodegenerative diseases, cancer, and cardiovascular diseases. Although a large number of drugs are available in the market for treatment of these diseases, however, the emphasis these days is on the exploitation of natural principles derived from plants. Most polyphenols show low in vivo bioavailability thus limiting their application for oral drug delivery. This low bioavailability could be associated with low aqueous solubility, first pass effect, metabolism in GIT, or irreversible binding to cellular DNA and proteins. Therefore, there is a need to devise strategies to improve oral bioavailability of polyphenols. Various approaches like nanosizing, self-microemulsifying drug delivery systems (SMEDDS), microencapsulation, complexation, and solid dispersion can be used to increase the bioavailability. This paper will highlight the various methods that have been employed till date for the solubility enhancement of various polyphenols so that a suitable drug delivery system can be formulated.

scholarly journals FORMULATION AND EVALUATION OF NIFEDIPINE SUSTAINED RELEASE TABLETS BY USING DIFFERENT POLYMERS

2019 ◽  
Vol 8 (5) ◽  
Author(s):  
Shraddha Pawan Pareek ◽  
Sunil Kumawat ◽  
Vijay Sharma ◽  
Devender Sharma ◽  
Devendra Singh Rathore
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Oral Delivery ◽  
Oral Drug Delivery ◽  
Pharmaceutical Products ◽  
Matrix Tablets ◽  
Oral Drug ◽  
Release Formulation ◽  
Therapeutic Benefits ◽  
Sustained Release Tablets

Oral drug delivery has been known for many years because the most generally utilized route of administration among all the routes that are explored for the general delivery of medication via various pharmaceutical products of different dosage forms.  The reason that the oral route achieved such quality could also be partly attributed to its simple administration moreover because the ancient belief that by oral administration the drug is well absorbed because the food stuffs that area unit eaten daily. In fact the event of a pharmaceutical product for oral delivery, no matter its physical kind involves variable extents of optimization of dose kind characteristics at intervals the inherent constraints of GI physiology.  The rationale for development of a extended release formulation of a drug is to enhance its therapeutic benefits, minimizing its side effects while improving the management of the diseased condition. The aim of the present investigation is to formulate and evaluate matrix tablets of Nifedipine using a mixture of polymers in view to sustain the drug release, reduce frequency of administration and improved patient compliance. In this research paper all evaluation parameter and stability studies also well discussed in well manner. Keyword: Matrix Tablets, Coating, Novel Drug Delivery System, Sustained Release Tablets

Potential cardio-protective agents: A Resveratrol review (2000-2019).

2020 ◽  
Vol 26 ◽  
Author(s):  
Chahinez Houacine ◽  
Iftikhar Khan ◽  
Sakib Saleem Yousaf
Keyword(s):  
Drug Delivery ◽  
Clinical Effect ◽  
Water Solubility ◽  
Oral Drug Delivery ◽  
Oral Drug ◽  
Protective Agent ◽  
Physiochemical Properties ◽  
Area Of Interest ◽  
Therapeutic Compounds

: With a 2030 projection of 23.6 million deaths per year the prevalence and severity of cardiovascular disease is at an astounding high. Thus, a definitive need for the identification of novel compounds with potential to prevent or treat the disease and associated states. Moreover, there is also an ever-increasing need for drug delivery systems (DDS) that cope with poor and ranging physiochemical properties of therapeutic compounds to achieve clinical effect. The usage of resveratrol (RES) is a growing area of interest with innumerate pieces of research evidencing the drug’s efficacy. This drug is however marred, its notably poor physiochemical properties (namely poor water solubility) limits its use for oral drug delivery. RES analogues however, potentially possess superior physiochemical characteristics offering a remedy for the aforementioned drawback. However, particulate based DDS are equally able to offer property amelioration and targeting. This review offers an extensive examination into the role of RES as a potential cardio protective agent. The prevalence and suitability of associated analogues and the role of nanotechnology in overcoming physicochemical boundaries, particularly through the development of nanoparticulate formulations, will be discussed in detail.

Fast Dissolution Electrospun Medicated Nanofibers for Effective Delivery of Poorly Water-Soluble Drugs

2021 ◽  
Vol 18 ◽  
Author(s):  
Yrysbaeva Aidana ◽  
Yibin Wang ◽  
Jie Li ◽  
Shuyue Chang ◽  
Ke Wang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Oral Delivery ◽  
Oral Drug Delivery ◽  
Drug Carriers ◽  
Water Soluble ◽  
Oral Drug ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Fast Dissolution

Background: Electrospinning is developing rapidly from an earlier laboratory method into an industrial process. The clinical applications are approached in various ways through electrospun medicated nanofibers. The fast-dissolving oral drug delivery system (DDS) among them is one of the most promising routes in the near future for commercial applications. Methods: Related papers are investigated, including the latest research results, on electrospun nanofiber-based fast-dissolution DDSs. Results: Several relative topics have been concluded: 1) the development of electrospinning, ranging from 1-fluid blending to multi-fluid process and potential applications in the formation of medicated nanofibers involving poorly water-soluble drugs; 2) Selection of appropriate polymer matrices and drug carriers for filament formation; 3) Types of poorly water-soluble drugs ideal for fast oral delivery; 4) The methods for evaluating fast-dissolving nanofibers; 5) The mechanisms that promote the fast dissolution of poorly water-soluble drugs by electrospun nanofibers; 6) the important issues for further development of electrospun medicated nanofibers as oral fast-dissolving drug delivery systems. Conclusions & Perspectives: The unique properties of electrospun-medicated nanofibers can be used as oral fast dissolving DDSs of poorly water-soluble drugs. However, some significant issues need to be investigated, such as scalable productions and solid dosage form conversions.

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