Mechanistic Insights into High Permeation Vesicle-Mediated Synergistic Enhancement of Transdermal Drug Permeation

Jain, Sanyog; Khare, P. K.; Date, Tushar; Katiyar, Sameer S.; Kushwah, Varun; Katariya, Mahesh; Swami, Rajan

doi:10.2217/nnm-2018-0519

Cited by 4 publications

(19 citation statements)

References 54 publications

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“…The skin has proven to be beneficial for both localized and systemic drug deliveries by showing various advantages, including 1) bypassing the hepatic first-pass effect, 2) minimizing changes in drug/natural product plasma levels, 3) allowing selective targ,eting 4) flexibility for controlledrelease profiles, 5) improved patient compliance, and 6) cost-effectiveness. [201][202][203] The stratum corneum allows for percutaneous absorption of drugs and natural products. It is 10 µm thick, keratinized epidermal cells that act as a rate limiting barrier for drug/natural products permeation, 204,205 thus restricting the entry of polar, big molecular weight substances.…”

Section: Challenges and Opportunities Of Natural Products In Transdermal/topical Delivery Systems And Their Safety Considerations For Skimentioning

confidence: 99%

Promising Natural Products in New Drug Design, Development, and Therapy for Skin Disorders: An Overview of Scientific Evidence and Understanding Their Mechanism of Action

Zaid¹,

Sekar²,

Bonam³

et al. 2022

DDDT

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The skin is the largest organ in the human body, composed of the epidermis and the dermis. It provides protection and acts as a barrier against external menaces like allergens, chemicals, systemic toxicity, and infectious organisms. Skin disorders like cancer, dermatitis, psoriasis, wounds, skin aging, acne, and skin infection occur frequently and can impact human life. According to a growing body of evidence, several studies have reported that natural products have the potential for treating skin disorders. Building on this information, this review provides brief information about the action of the most important in vitro and in vivo research on the use of ten selected natural products in inflammatory, neoplastic, and infectious skin disorders and their mechanisms that have been reported to date. The related studies and articles were searched from several databases, including PubMed, Google, Google Scholar, and ScienceDirect. Ten natural products that have been reported widely on skin disorders were reviewed in this study, with most showing anti-inflammatory, antioxidant, anti-microbial, and anti-cancer effects as the main therapeutic actions. Overall, most of the natural products reported in this review can reduce and suppress inflammatory markers, like tumor necrosis factor-alpha (TNF-α), scavenge reactive oxygen species (ROS), induce cancer cell death through apoptosis, and prevent bacteria, fungal, and virus infections indicating their potentials. This review also highlighted the challenges and opportunities of natural products in transdermal/topical delivery systems and their safety considerations for skin disorders. Our findings indicated that natural products might be a low-cost, welltolerated, and safe treatment for skin diseases. However, a larger number of clinical trials are required to validate these findings. Natural products in combination with modern drugs, as well as the development of novel delivery mechanisms, represent a very promising area for future drug discovery of these natural leads against skin disorders.

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Section: Challenges and Opportunities Of Natural Products In Transdermal/topical Delivery Systems And Their Safety Considerations For Skimentioning

confidence: 99%

Promising Natural Products in New Drug Design, Development, and Therapy for Skin Disorders: An Overview of Scientific Evidence and Understanding Their Mechanism of Action

Zaid¹,

Sekar²,

Bonam³

et al. 2022

DDDT

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show abstract

“…HPVs were prepared by thin film hydration method as per our previous publication. 16 In brief, accurately weighed quantities of the Phospholipon 90H and SCOPE in a ratio of 8:2 (% w/w) were dissolved in ethanol along with DTX. The solvent was evaporated under reduced pressure using rotary evaporator to form a uniform film and further dried in vacuum oven at 40 °C to ensure residual solvent removal.…”

Section: Methodsmentioning

confidence: 99%

“…The spreadability of formulation was measured using the acrylic plate method. 16 Spreading of gel as a function of weight was measured by placing 1 g of sample between the center of plate. Increase in the diameter as a function of spreadability was observed by incrementally adding weights of 25, 50, and 100 g for 5 min.…”

Section: Methodsmentioning

confidence: 99%

“…The samples were analyzed for DTX content using a validated HPLC method. 16 3.4.2. Dermal Drug Distribution Analysis.…”

Section: Methodsmentioning

confidence: 99%

“…We discovered that HPV-mediated transdermal permeation enhancement was a cumulative impact of enhanced vesicle deformability, improved vesicle membrane fluidity, better skin fluidization, and synergistic permeation enhancement action of SCOPE components. 16 In the present work, we have explored the possibility of localized transdermal delivery of DTX using HPVs for topical chemotherapy in breast cancer.…”

Section: Introductionmentioning

confidence: 99%

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Exploring the Promising Potential of High Permeation Vesicle-Mediated Localized Transdermal Delivery of Docetaxel in Breast Cancer To Overcome the Limitations of Systemic Chemotherapy

et al. 2020

Self Cite

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The currently available systemic chemotherapy for treating breast cancer often results in serious systemic side effects and compromises patient compliance. The distinct anatomical features of human breasts (e.g., embryological origin of breast skin, highly developed internal lymphatic and venous circulation, and the presence of mammary fat layers) help in preferential accumulation of drugs into breasts after topical application on breast region. This unique feature is termed as localized transdermal delivery which could be utilized for effectively delivering anticancer agents to treat breast cancer and reducing the systemic side effects by limiting their presence in blood. However, the clinical effectiveness of this drug delivery approach is highly limited by barrier properties of skin reducing the permeation of anticancer drugs. In the present work, we have developed high permeation vesicles (HPVs) using phospholipids and synergistic combination of permeation enhancers (SCOPE) to improve the skin permeation of drugs. Docetaxel (DTX) was used as a model drug for hypothesis testing. The optimized SCOPE mixture composed of sodium oleate/sodium lauryl ether sulfate/propylene glycol in 64:16:20% w/w ratio. DTX HPVs were prepared using phospholipid: SCOPE, 8:2% w/w ratio. DTX HPVs exhibited as a uniform deformable vesicles with size range 124.2 ± 7.6 nm, significantly improved skin permeation profile, and sustained drug release until 48 h. Superior vesicle deformability, better vesicle membrane fluidization, and SCOPE mediated enhancement in skin fluidization were the prime factors behind enhancement of DTX permeation. The improved cellular uptake, reduced IC50 values, and higher apoptotic index of DTX HPVs in MCF-7 and MDA-MB-231 cells ensured the therapeutic effectiveness of HPV based therapy. Also, HPVs were found to be predominantly internalized inside cells through clathrin and caveolae-dependent endocytic pathways. Bioimaging analysis in mice confirmed the tumor penetration potential and effective accumulation of HPVs inside tumors after topical application. In vivo studies were carried out in comparison with marketed intravenous DTX injection (Taxotere) to compare the effectiveness of topical chemotherapy. The topical application of DTX HPV gel in tumor bearing mice resulted in nearly 4-fold tumor volume reduction which was equivalent to intravenous Taxotere therapy. Toxicity analysis of DTX HPV gel in comparison with intravenous Taxotere dosing showcased remarkably lower levels of toxicity biomarkers (aspartate transaminase (AST), alanine transaminase (ALT), blood urea nitrogen (BUN), and creatinine), indicating improved safety of topical chemotherapy. Overall results warranted the effectiveness of topical DTX chemotherapy to reduce tumor burden with substantially reduced risk of systemic toxicities in breast cancer.

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Bile salts: unlocking the potential as bio-surfactant for enhanced drug absorption

Chakravarthy,

Popli,

Challa

et al. 2024

J Nanopart Res

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Mechanistic Insights into High Permeation Vesicle-Mediated Synergistic Enhancement of Transdermal Drug Permeation

Cited by 4 publications

References 54 publications

Promising Natural Products in New Drug Design, Development, and Therapy for Skin Disorders: An Overview of Scientific Evidence and Understanding Their Mechanism of Action

Promising Natural Products in New Drug Design, Development, and Therapy for Skin Disorders: An Overview of Scientific Evidence and Understanding Their Mechanism of Action

Exploring the Promising Potential of High Permeation Vesicle-Mediated Localized Transdermal Delivery of Docetaxel in Breast Cancer To Overcome the Limitations of Systemic Chemotherapy

Bile salts: unlocking the potential as bio-surfactant for enhanced drug absorption

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