Recent Advances in Drug Delivery Strategies for Improved Therapeutic Efficacy of Efavirenz

2020 ◽  
Vol 14 (2) ◽  
pp. 119-127
Author(s):  
Mitali Patel ◽  
Ruhi Shah ◽  
Krutika Sawant

Background: Efavirenz, an anti-HIV agent, has a noticeable place in the HAART regimen for the treatment and maintenance therapy of AIDS. However, its poor water solubility accounts for hindered absorption and bio-distribution upon administration. This results in its low and variable bioavailability. To circumvent these limitations, various novel formulations of Efavirenz have been investigated in order to mitigate its drawbacks and draw out its maximum therapeutic effect. Methods: Numerous formulations explored to overcome the drawbacks of Efavirenz include modified/ controlled-release tablets, solid dispersions, polymeric nanoparticles, dendrimers, surface-engineered nanoparticles and various other nanoformulations. Moreover, combinatorial formulations of Efavirenz with other Anti-HIV drugs have also been reported to overcome the problem of Drug-Resistance. Results: The nanoformulation based strategies, owing to their ability to provide controlled release profile and targeted drug delivery were found to augment bioavailability, therapeutic efficacy and reduce the side effects of the Efavirenz. Conclusion: This review pivots around the challenges and recent advances in the delivery of Efavirenz with particular emphasis on novel formulations including its patents.

2019 ◽  
Vol 10 (8) ◽  
pp. 527-550 ◽  
Author(s):  
Vahid Taghipour-Sabzevar ◽  
Tahere Sharifi ◽  
Mehrdad Moosazadeh Moghaddam

In recent decades, many novel methods by using nanoparticles (NPs) have been investigated for diagnosis, drug delivery and treatment of cancer. Accordingly, the potential of NPs as carriers is very significant for the delivery of anticancer drugs, because cancer treatment with NPs has led to the improvement of some of the drug delivery limitations such as low blood circulation time and bioavailability, lack of water solubility, drug adverse effect. In addition, the NPs protect drugs against enzymatic degradation and can lead to the targeted and/or controlled release of the drug. The present review focuses on the potential of NPs that can help the targeted and/or controlled delivery of anticancer agents for cancer therapy.


Author(s):  
Garima Joshi ◽  
Krutika Sawant ◽  
Mitali Patel ◽  
Deepak Chaudhary

: Nanotechnology is one of the emerging fields in the drug delivery for targeting the drug to the site of action. The polymeric nanoparticles as drug delivery systems have gained importance for the last few decades. They offer advantages over liposomes, dendrimers, emulsions etc. Surface engineering of polymeric nanoparticles is widely utilized to effectively target the cells in various diseases such as cancer, HIV infection. Surface modified nanoparticles offer various advantages such as targeted drug delivery, reduction in side effects, dose reductionand improved therapeutic efficacy. Moreover, they can aid in improving physical and biochemical properties, pharmacokinetic and pharmacodynamic profiles of drug. Surface modified polymeric nanoparticles can provide targeted delivery of drugs into specific cells, especially when targets are intracellular localized. This approach would be more advantageous for the delivery of various anticancer, anti inflammatory, anti HIV drugs for more effective therapy. This review focuses on the techniques used for fabrication of polymeric nanoparticles, material used for surface modification and their applications.


2020 ◽  
Vol 22 (1) ◽  
pp. 340
Author(s):  
Ilya Nifant’ev ◽  
Andrei Siniavin ◽  
Eduard Karamov ◽  
Maxim Kosarev ◽  
Sergey Kovalchuk ◽  
...  

Despite the world’s combined efforts, human immunodeficiency virus (HIV), the causative agent of AIDS, remains one of the world’s most serious public health challenges. High genetic variability of HIV complicates the development of anti-HIV vaccine, and there is an actual clinical need for increasing the efficiency of anti-HIV drugs in terms of targeted delivery and controlled release. Tenofovir (TFV), a nucleotide-analog reverse transcriptase inhibitor, has gained wide acceptance as a drug for pre-exposure prophylaxis or treatment of HIV infection. In our study, we explored the potential of tenofovir disoproxil (TFD) adducts with block copolymers of poly(ethylene glycol) monomethyl ether and poly(ethylene phosphoric acid) (mPEG-b-PEPA) as candidates for developing a long-acting/controlled-release formulation of TFV. Two types of mPEG-b-PEPA with numbers of ethylene phosphoric acid (EPA) fragments of 13 and 49 were synthesized by catalytic ring-opening polymerization, and used for preparing four types of adducts with TFD. Antiviral activity of [mPEG-b-PEPA]TFD or tenofovir disoproxil fumarate (TDF) was evaluated using the model of experimental HIV infection in vitro (MT-4/HIV-1IIIB). Judging by the values of the selectivity index (SI), TFD exhibited an up to 14-fold higher anti-HIV activity in the form of mPEG-b-PEPA adducts, thus demonstrating significant promise for further development of long-acting/controlled-release injectable TFV formulations.


2016 ◽  
Vol 8 (9) ◽  
pp. 956-967 ◽  
Author(s):  
Lin Li ◽  
Lu Tian ◽  
Wenjing Zhao ◽  
Yingqi Li ◽  
Binsheng Yang

A successful drug delivery device for cancer chemotherapy should ideally be able to load drugs highly, bring the drug preferentially into tumor cells and reduce its distribution in normal tissue to enhance therapeutic efficacy.


2015 ◽  
Vol 3 (39) ◽  
pp. 7707-7717 ◽  
Author(s):  
Jinyan Lin ◽  
Yanxiu Li ◽  
Yang Li ◽  
Fei Cui ◽  
Fei Yu ◽  
...  

Self-targeted, bacillus-shaped, and controlled-release methotrexate prodrug polymeric nanoparticles for highly efficient cancer chemotherapy: more elongated is better.


Drug Delivery ◽  
2020 ◽  
Vol 27 (1) ◽  
pp. 180-190 ◽  
Author(s):  
Wanfu Men ◽  
Peiyao Zhu ◽  
Siyuan Dong ◽  
Wenke Liu ◽  
Kun Zhou ◽  
...  

2019 ◽  
Vol 138 ◽  
pp. 99-110 ◽  
Author(s):  
Margaret Siyawamwaya ◽  
Lisa C. du Toit ◽  
Pradeep Kumar ◽  
Yahya E. Choonara ◽  
Pierre P.P.D. Kondiah ◽  
...  

2020 ◽  
Vol 22 (1) ◽  
pp. 115
Author(s):  
Magdalena Paczkowska-Walendowska ◽  
Natalia Rosiak ◽  
Ewa Tykarska ◽  
Katarzyna Michalska ◽  
Anita Płazińska ◽  
...  

Progressive increase in bacterial resistance has caused an urgent need to introduce new antibiotics, one of them being oxazolidinones with their representative tedizolid. Despite the broad spectrum of activity of the parent tedizolid, it is characterized by low water solubility, which limits its use. The combination of the active molecule with a multifunctional excipient, which is cyclodextrins, allows preservation of its pharmacological activity and modification of its physicochemical properties. Therefore, the aim of the study was to change the dissolution rate and permeability through the model membrane of tedizolid by formation of solid dispersions with a cyclodextrin. The research included identification of tedizolid-hydroxypropyl-β-cyclodextrin (tedizolid/HP-β-CD) inclusion complex by thermal method (Differential Scanning Colorimetry), spectroscopic methods (powder X-ray diffraction, Fourier-Transform Infrared spectroscopy), and molecular docking. The second part of the research concerned the physicochemical properties (dissolution and permeability) and the biological properties of the system in terms of its microbiological activity. An increase in the dissolution rate was observed in the presence of cyclodextrin, while maintaining a high permeation coefficient and high microbiological activity. The proposed approach is an opportunity to develop drug delivery systems used in the treatment of resistant bacterial infections, in which, in addition to modifying the physicochemical properties caused by cyclodextrin, we observe a favorable change in the pharmacological potential of the bioactives.


2014 ◽  
Vol 21 (11) ◽  
pp. 1102-1120 ◽  
Author(s):  
Ashaben Patel ◽  
Mitesh Patel ◽  
Xiaoyan Yang ◽  
Ashim Mitra

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