scholarly journals Improved Dermal and Transdermal Delivery of Curcumin with SmartFilms and Nanocrystals

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1633
Author(s):  
Ralph W. Eckert ◽  
Sabrina Wiemann ◽  
Cornelia M. Keck
Keyword(s):  
Drug Delivery ◽  
Transdermal Delivery ◽  
Aqueous Solubility ◽  
Local Concentration ◽  
Active Compounds ◽  
Drug Products ◽  
Dermal Penetration ◽  
Penetration Mechanism ◽  
Poorly Soluble ◽  
Transdermal Penetration

Poor aqueous solubility of active compounds is a major issue in today’s drug delivery. In this study the smartFilm-technology was exploited to improve the dermal penetration efficacy of a poorly soluble active compound (curcumin). Results were compared to the dermal penetration efficacy of curcumin from curcumin bulk suspensions and nanocrystals, respectively. The smartFilms enabled an effective dermal and transdermal penetration of curcumin, whereas curcumin bulk- and nanosuspensions were less efficient when the curcumin content was similar to the curcumin content in the smartFilms. Interestingly, it was found that increasing numbers of curcumin particles within the suspensions increased the passive dermal penetration of curcumin. The effect is caused by an aqueous meniscus that is created between particle and skin if the dispersion medium evaporates. The connecting liquid meniscus causes a local swelling of the stratum corneum and maintains a high local concentration gradient between drug particles and skin. Thus, leading to a high local passive dermal penetration of curcumin. The findings suggest a new dermal penetration mechanism for active compounds from nano-particulate drug delivery systems, which can be the base for the development of topical drug products with improved penetration efficacy in the future.

scholarly journals Hair Follicle Targeting and Dermal Drug Delivery with Curcumin Drug Nanocrystals—Essential Influence of Excipients

Nanomaterials ◽  
2020 ◽  
Vol 10 (11) ◽  
pp. 2323
Author(s):  
Olga Pelikh ◽  
Cornelia M. Keck
Keyword(s):  
Drug Delivery ◽  
Hair Follicle ◽  
Aqueous Solubility ◽  
Hair Follicles ◽  
Passive Diffusion ◽  
Dermal Penetration ◽  
Poorly Soluble ◽  
Long Acting ◽  
Dermal Drug Delivery ◽  
Dermal Application

Many active pharmaceutical ingredients (API) possess poor aqueous solubility and thus lead to poor bioavailability upon oral administration and topical application. Nanocrystals have a well-established, universal formulation approach to overcome poor solubility. Various nanocrystal-based products have entered the market for oral application. However, their use in dermal formulations is relatively novel. Previous studies confirmed that nanocrystals are a superior formulation principle to improve the dermal penetration of poorly soluble API. Other studies showed that nanocrystals can also be used to target the hair follicles where they create a drug depot, enabling long acting drug therapy with only one application. Very recent studies show that also the vehicle in which the nanocrystals are incorporated can have a tremendous influence on the pathway of the API and the nanocrystals. In order to elucidate the influence of the excipient in more detail, a systematic study was conducted to investigate the influence of excipients on the penetration efficacy of the formulated API and the pathway of nanocrystals upon dermal application. Results showed that already small quantities of excipients can strongly affect the passive dermal penetration of curcumin and the hair follicle targeting of curcumin nanocrystals. The addition of 2% ethanol promoted hair follicle targeting of nanocrystals and hampered passive diffusion into the stratum corneum of the API, whereas the addition of glycerol hampered hair follicle targeting and promoted passive diffusion. Propylene glycol was found to promote both pathways. In fact, the study proved that formulating nanocrystals to improve the bioefficacy of poorly soluble API upon dermal application is highly effective. However, this is only true, if the correct excipient is selected for the formulation of the vehicle. The study also showed that excipients can be used to allow for a targeted dermal drug delivery, which enables to control if API should be delivered via passive diffusion and/or as drug reservoir by depositing API in the hair follicles.

Self-microemulsion Technology for Water-insoluble Drug Delivery

2019 ◽  
Vol 15 (6) ◽  
pp. 576-588 ◽  
Author(s):  
Beibei Yan ◽  
Yu Gu ◽  
Juan Zhao ◽  
Yangyang Liu ◽  
Lulu Wang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Aqueous Solubility ◽  
Delivery Systems ◽  
Poorly Soluble Drugs ◽  
New Chemical Entities ◽  
Poorly Soluble ◽  
Water Insoluble Drug ◽  
Semi Solid ◽  
Solidification Technology

: According to the drug discovery, approximately 40% of the new chemical entities show poor bioavailability due to their low aqueous solubility. In order to increase the solubility of the drugs, self-micro emulsifying drug delivery systems (SMEDDS) are considered as an ideal technology for enhancing the permeability of poorly soluble drugs in GI membranes. The SMEDDS are also generally used to enhance the oral bioavailability of the hydrophobic drugs. At present, most of the self-microemulsion drugs are liquid dosage forms, which could cause some disadvantages, such as the low bioavailability of the traditional liquid SMEDDS. Therefore, solid self-micro emulsifying drug delivery systems (S-SMEDDS) have emerged widely in recent years, which were prepared by solidifying a semi-solid or liquid self-emulsifying (SE) ingredient into a powder in order to improve stability, treatment and patient compliance. The article gives a comprehensive introduction of the study of SMEDDS which could effectively tackle the problem of the water-insoluble drug, especially the development of solidification technology of SMEDDS. Finally, the present challenges and the prospects in this field were also discussed.

scholarly journals Self Emulsifying Drug Delivery System: A Recent Approach

2019 ◽  
Vol 31 (4) ◽  
pp. 751-759 ◽  
Author(s):  
Sabitri Bindhani ◽  
S. Mohapatra ◽  
R.K. Kar
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Bioavailability ◽  
Oral Absorption ◽  
Scale Up ◽  
Aqueous Solubility ◽  
Oral Drug ◽  
Recent Approach ◽  
Poorly Soluble

In recent years, nearly 40 % newer drugs compounds are hydrophobic in nature, which is a major challenge now-a-days for oral drug delivering due to low aqueous solubility. Lipid based drug delivery system is one of the favourable approach for poorly soluble compounds which can improve the drug absorption and oral bioavailability. Due to ion-pairing with appropriate surfactant and co-surfactant the macromolecular drug molecular oil droplet being found in the gut flow oral absorption which sufficiently stable towards lipase. Due to the formation of emulsified drug in micron level, it can efficiently endow the oral bioavailability. Several comprehensive papers have been published in the literature illustration diverse type of lipid based formulation with recent advancements. This article is based on an exhaustive and updated review on newer technology which out line an explicit discussion on its formulations and industrial scale up.

Enhancement the Dissolution Rate and Solubility of Poorly Soluble Drugs: Review

2013 ◽  
Vol 701 ◽  
pp. 234-238 ◽  
Author(s):  
Mubarak Abdullah Saleh ◽  
Salam A. Mohammed ◽  
Ezzat C Abdullah ◽  
Laith A. Hashim
Keyword(s):  
Drug Delivery ◽  
Chemical Composition ◽  
Active Pharmaceutical Ingredient ◽  
Nucleation Mechanism ◽  
Rapid Freezing ◽  
Poorly Soluble Drugs ◽  
Pharmaceutical Development ◽  
Drug Products ◽  
Poorly Soluble ◽  
As Solubility

The use of reduction and nucleation technologies in nanosize active pharmaceutical ingredient (API) is as an enabling to bring improved drug products to the marketplace demand as well as for improved drug delivery. nanoPharmaceutical field represents a hopeful set of pharmaceutical materials offering the prospect of better alternatives to optimize drug physical properties and biopharmaceutical issues such as solubility, stability and bioavailability in pharmaceutical development without changing the chemical composition of the API, thereby, giving new patentable solid forms. With physically improved solid API may impact the the pharmaceutical intellectual property landscape. Nanoparticle formation is achievable in many ways, although primarily through particle reduction or through manipulation of the nucleation mechanism. Keywords: active pharmaceutical ingredient; drug delivery; ultra rapid freezing.

Recent Advances in Self-Emulsifying Drug Delivery Systems

2015 ◽  
Vol 8 (1) ◽  
pp. 2693-2697
Author(s):  
Amol S Deshmukh
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Aqueous Solubility ◽  
Oral Route ◽  
Delivery Systems ◽  
Novel Technologies ◽  
Oral Formulations ◽  
Modern Drug ◽  
New Chemical Entities ◽  
Poorly Soluble

Oral route has always been preferred route for formulators and has dominated over other routes of administrations. But major problem encountered in oral formulations (as estimated more than 50 % of oral formulations are found to be poorly aqueous soluble), is low bioavailability, giving rise to further problems like, high inter and intra subject variability, lack of dose uniformity and finally leading to therapeutic failure. Approximately 40% of new chemical entities exhibit poor aqueous solubility and present a major challenge to modern drug delivery system, because of their low bioavailability. Particularly for BCS class II substances, the bioavailability may be enhanced by increasing the solubility and dissolution rate of the drug in the gastro-intestinal fluids. The newer and novel technologies developed in recent year for troubleshooting such above problems. This review describes an overview of SEDDS as a capable approach to effectively capture the problem of poorly soluble molecules and give the novel approaches for evaluation of the SEDDS. Self-emulsifying drug delivery systems (SEDDS) are isotropic mixtures of drug, lipids and surfactants, usually with one or more hydrophilic co-solvents or co-emulsifiers.  

scholarly journals Self-Emulsifying Formulations: A Pharmaceutical Review

2020 ◽  
Vol 10 (3) ◽  
pp. 231-240
Author(s):  
Chukwuma Agubata
Keyword(s):  
Drug Delivery ◽  
Oral Delivery ◽  
Drug Delivery Systems ◽  
Aqueous Solubility ◽  
Oral Route ◽  
Concept Design ◽  
Lipophilic Drugs ◽  
Oil In Water ◽  
Poorly Soluble ◽  
Mild Agitation

The oral route of drug delivery is commonly utilized for administration of medicines and is particularly preferred for the treatment of many chronic diseases which require continuous ingestion over a reasonably prolonged period of time. However the oral delivery of lipophilic drugs presents a major obstacle because of their low aqueous solubility. The aqueous solubility of a drug is a crucial determinant of its dissolution rate, absorption and bioavailability. Drugs with relatively high intrinsic lipophilicity can be dissolved in appropriate mixtures of oils/lipids, surfactants, cosolvents which can rapidly form oil-in-water (o/w) fine emulsions when dispersed in aqueous phase under mild agitation or mixing. These isotropic self-emulsifying formulations or self-emulsifying drug delivery systems are effective for delivery of poorly soluble, lipophilic drugs by dispersing the drugs within fine oil droplets in emulsions and this solubilization of drugs can then improve its absorption, bioavailability and therapeutic efficacy. The present paper reviews the concept, design, formulation, characterization and applications of self-emulsifying formulations. Keywords: Self-Emulsifying Formulations, lipophilicity, emulsions

scholarly journals Bioavailability Enhancement Techniques for Poorly Soluble Drugs: A Review

2020 ◽  
Vol 8 (2) ◽  
pp. 75-78
Author(s):  
Ravi Gupta ◽  
Vidhi Jain ◽  
Jagdish Chand Nagar ◽  
Aadil Ansari ◽  
Kapil Sharma ◽  
...  
Keyword(s):  
Aqueous Solubility ◽  
New Drugs ◽  
Drug Dissolution ◽  
Formulation Development ◽  
Bioavailability Enhancement ◽  
Novel Technologies ◽  
Drug Products ◽  
Bcs Class Ii ◽  
Poorly Soluble ◽  
Extent Of Absorption

Bioavailability is defined as the rate and extent of absorption of unchanged drug from its dosage form. The oral bioavailability of drugs with poor solubility and reasonable permeability is limited by the drug dissolution step from drug products. Low aqueous solubility is the major problem encountered with formulation development of new drugs. The article briefly highlights traditional and novel techniques that are used for solubility enhancement of BCS Class II drugs are discussed in this article. The Traditional techniques include use of co-solvents, hydrotrophy, micronization, change in dielectric constant of solvent, amorphous forms, chemical modification of drug, use of surfactants etc. Novel technologies are size reduction technologies, lipid based delivery system, micellar technologies, solid dispersion and many more.    

Solubility Enhancement of Poorly Soluble Drug Simvastatin by Solid Dispersion Technique

2016 ◽  
Vol 2 (2) ◽  
pp. 91-95
Author(s):  
Neelima Rani T ◽  
Pavani A ◽  
Sobhita Rani P ◽  
Srilakshmi N
Keyword(s):  
Dissolution Rate ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Onset Of Action ◽  
Kneading Method ◽  
Wetting Property ◽  
Poorly Soluble ◽  
Dispersion Technique ◽  
Low Solubility

This study aims to formulate solid dispersions (SDs) of Simvastatin (SIM) to improve the aqueous solubility, dissolution rate and to facilitate faster onset of action. Simvastatin is a BCS class II drug having low solubility & therefore low oral bioavailability. In the present study, SDs of simvastatin different drug-carrier ratios were prepared by kneading method. The results showed that simvastatin solubility & dissolution rate enhanced with polymer SSG in the ratio 1:7 due to increase in wetting property or possibly may be due to change in crystallinity of the drug.

Self Microemulsifying Nutraceutical and Drug Delivery Systems

2014 ◽  
Vol 7 (3) ◽  
pp. 2520-2528 ◽  
Author(s):  
Vikrant P Wankhade ◽  
Nivedita S Kale ◽  
K.K Tapar
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ternary Phase Diagram ◽  
Aqueous Solubility ◽  
Oral Formulation ◽  
Water Soluble ◽  
Drug Dissolution ◽  
The Novel ◽  
Peristaltic Movement

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.

Identifying underlying issues related to the inactive excipients of transfersomes based drug delivery system

2020 ◽  
Vol 26 ◽  
Author(s):  
Drashti Patel ◽  
Bappaditya Chatterjee
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Transdermal Delivery ◽  
Systemic Availability ◽  
Drug Penetration ◽  
Skin Damage ◽  
Variable Effect ◽  
Practical Factors ◽  
Edge Activator

: Transfersomes are bilayer vesicles composed of phospholipid and edge-activators, which are mostly surfactant. Transfersomes based drug delivery system has gained a lot of interest of the pharmaceutical researchers for their ability to improve drug penetration and permeation through the skin. Transdermal drug delivery via transfersomes has the potential to overcome the challenge of low systemic availability. However, this complex vesicular system has different issues to consider for developing a successful transdermal delivery system. One of the major ingredients, phospholipid has versatile sources and variable effect on the vesicle size and drug entrapment in transfersomes. The other one termed as edge-activator or surfactant has some crucial consideration of skin damage and toxicity depending upon its type and concentration. A complex interaction between type and concentration of phospholipid and surfactant was observed, which affect the physicochemical properties of transfersomes. This review focuses on the practical factors related to these two major ingredients such as phospholipid and surfactant. The origin, purity, desired concentration, the susceptibility of degradation, etc. are the important factors for selecting phospholipid. Regarding surfactants, the major aspects are type and desired concentration. A successful development of transfersomes based drug delivery system depends on the proper considerations of these factors and practical aspects.

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