scholarly journals Emulsion-Based Multicompartment Vaginal Drug Carriers: From Nanoemulsions to Nanoemulgels

2021 ◽  
Vol 22 (12) ◽  
pp. 6455
Author(s):  
Michał Smoleński ◽  
Bożena Karolewicz ◽  
Anna M. Gołkowska ◽  
Karol P. Nartowski ◽  
Katarzyna Małolepsza-Jarmołowska

In order to overcome the limitations associated with vaginal administration of drugs, e.g., the short contact time of the drug form with the mucosa or continuous carrier wash-out, the development of new carriers for gynecological use is necessary. Furthermore, high individual anatomical and physiological variability resulting in unsatisfactory therapeutic efficacy of lipophilic active substances requires application of multicompartment drug delivery systems. This manuscript provides an up-to-date comprehensive review of the literature on emulsion-based vaginal dosage forms (EVDF) including macroemulsions, microemulsions, nanoemulsions, multiple emulsions and self-emulsifying drug delivery systems. The first part of the paper discusses (i) the influence of anatomical-physiological conditions on therapeutic efficacy of drug forms after local and systemic administration, (ii) characterization of EVDF components and the manufacturing techniques of these dosage forms and (iii) methods used to evaluate the physicochemical and pharmaceutical properties of emulsion-based vaginal dosage forms. The second part of the paper presents (iv) the results of biological and in vivo studies as well as (v) clinical evaluation of EVDF safety and therapeutic efficacy across different indications.

Nano LIFE ◽  
2016 ◽  
Vol 06 (03n04) ◽  
pp. 1642002 ◽  
Author(s):  
Fei Liu ◽  
Yuan Sun ◽  
Chen Kang ◽  
Hongyan Zhu

Pegylation, as a simple procedure to attach hydrophilic polyethylene glycol (PEG) onto therapeutic molecule or drug carriers has been utilized widely to deliver small molecules, proteins and peptides. It was first reported in 1970s by Dr. Frank Davis of Rutgers University and Dr. Abuchowsky in the studies of PEG modified albumin and catalase. The significance of this method at that time was able to successfully modify the enzyme with better hydrophilicity but also keep the enzymatic activity. The employment of PEG has provided superior stability of drug delivery systems (DDS) and enhanced the circulation time in vivo. Simple conjugation of PEG chains with various molecular weights enables the possibility to regulate the properties of desired DDS and led to important contribution in targeting therapy and diagnosis. Pegylation has been reported to be able to protect peptides by shielding antigenic epitopes from reticuloendothelial (RES) clearance and avoid enzymes being recognized by immune system and avoid early degradation. In addition, utilization of PEG in DDS are reported with enhanced delivery efficiency, prolonged circulation time and improved stability, especially active enzymes and peptides drug delivery. In this paper, we will conclude current studies about Pegylated DDS and their biomedical applications from both in vitro and in vivo studies.


2018 ◽  
Vol 14 (5) ◽  
pp. 432-439 ◽  
Author(s):  
Juliana M. Juarez ◽  
Jorgelina Cussa ◽  
Marcos B. Gomez Costa ◽  
Oscar A. Anunziata

Background: Controlled drug delivery systems can maintain the concentration of drugs in the exact sites of the body within the optimum range and below the toxicity threshold, improving therapeutic efficacy and reducing toxicity. Mesostructured Cellular Foam (MCF) material is a new promising host for drug delivery systems due to high biocompatibility, in vivo biodegradability and low toxicity. Methods: Ketorolac-Tromethamine/MCF composite was synthesized. The material synthesis and loading of ketorolac-tromethamine into MCF pores were successful as shown by XRD, FTIR, TGA, TEM and textural analyses. Results: We obtained promising results for controlled drug release using the novel MCF material. The application of these materials in KETO release is innovative, achieving an initial high release rate and then maintaining a constant rate at high times. This allows keeping drug concentration within the range of therapeutic efficacy, being highly applicable for the treatment of diseases that need a rapid response. The release of KETO/MCF was compared with other containers of KETO (KETO/SBA-15) and commercial tablets. Conclusion: The best model to fit experimental data was Ritger-Peppas equation. Other models used in this work could not properly explain the controlled drug release of this material. The predominant release of KETO from MCF was non-Fickian diffusion.


2012 ◽  
Vol 430 (1-2) ◽  
pp. 276-281 ◽  
Author(s):  
Yiguang Jin ◽  
Yanju Lian ◽  
Lina Du ◽  
Shuangmiao Wang ◽  
Chang Su ◽  
...  

2021 ◽  
Vol 28 ◽  
Author(s):  
Diego Arauna ◽  
Sekar Vijayakumar ◽  
Esteban Durán-Lara

Background: Drug delivery systems such as hydrogels have become relevant in cardiovascular and metabolic therapies due to their sustained and controlled release properties of drugs, versatile polymer structures, safety and biodegradability. Results: The literature presented demonstrates that a hydrogel-based controlled release system increases the therapeutic efficacy in different components of the metabolic syndrome. Hypertension has been the most explored component with advances in vitro and murine models. However, clinical evidence in humans is scarce, and more translational studies are needed. Hydrogel-based systems for diabetes, obesity, and dyslipidemia have been little explored. Observations mainly demonstrated an increase in therapeutic efficacy, in vitro and in vivo, for the use of insulin, leptin, and natural components, such as epigallocatechin gallate. In all cases, the hydrogel systems achieve better plasma levels of the loaded compound, higher bioavailability, and low cytotoxicity; compared to conventional systems. Also, the evidence existing suggests that the development of an injectable hydrogel system for controlled release of drugs or therapeutic compounds is presented as an attractive option for MeS treatment, due to the possibility of sustained pharmacological release, no need for repeated doses, and a safe administration route. Conclusion: The following review aims to evaluate the use of the hydrogel systems in the therapy of diabetes, obesity, hypertension, and dyslipidemia, which are the main components of metabolic syndrome.


2020 ◽  
Vol 15 (8) ◽  
pp. 679-698 ◽  
Author(s):  
Gratiela G Pircalabioru ◽  
Mariana-Carmen Chifiriuc

Biofilms are highly tolerant to antimicrobial agents and adverse environmental conditions being important reservoirs for chronic and hard-to-treat infections. Nanomaterials exhibit microbiostatic/microbicidal/antipathogenic properties and can be also used for the delivery of antibiofilm agents. However, few of the many promising leads offered by nanotechnology reach clinical studies and eventually, become available to clinicians. The aim of this paper was to review the progress and challenges in the development of nanotechnology-based antibiofilm drug-delivery systems. The main identified challenges are: most papers report only in vitro studies of the activity of different nanoformulations; lack of standardization in the methodological approaches; insufficient collaboration between material science specialists and clinicians; paucity of in vivo studies to test efficiency and safety.


2018 ◽  
Vol 8 (5-s) ◽  
pp. 87-93
Author(s):  
AS Bansode ◽  
K Sarvanan

Novel drug delivery systems (NDDS) are the key area of pharmaceutical research and Development. The reason is relatively low development cost and time required for introducing a NDDS as compared to new chemical entity. Many conventional drug delivery systems have been designed to modulate the release a drug over an extended period of a time. Various designs are available to control or modulate the drug release from a dosage forms. Majority of oral CR dosage forms fall in the category of matrix, reservoir or osmotic systems. Osmotically controlled drug delivery systems (OCDDS) is one of the most promising drug delivery technology that use osmotic pressure as a driving force for controlled delivery of active agents. Drug release from OCDDS is independent of pH and hydrodynamic conditions of the body because of the semipermeable nature of the Rate controlling membrane and the design of deliver orifice used in osmotic systems, so a high degree of In vitro/In vivo correlation is achieved. Osmotic drug delivery systems release the drug with the zero order kinetics which does not depend on the initial concentration and the physiological factors of GIT. This review brings out new technologies, fabrication and recent clinical research in osmotic drug delivery. Keywords: Osmotic, Matrix, Reservoir, Fabrication


RSC Advances ◽  
2015 ◽  
Vol 5 (36) ◽  
pp. 28219-28227 ◽  
Author(s):  
Olga Martinho ◽  
Natália Vilaça ◽  
Paulo J. G. Castro ◽  
Ricardo Amorim ◽  
António M. Fonseca ◽  
...  

Y and MOR zeolites were used as a host for the temozolomide (TMZ). Y presented toxicity to glioblastoma cancer cells in contrast to MOR. Higher potentiation of TMZ was obtained with MOR in comparison to free TMZ bothin vitroandin vivo.


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