scholarly journals Solid Lipid Nanoparticles as Formulative Strategy to Increase Oral Permeation of a Molecule Active in Multidrug-Resistant Tuberculosis Management

Pharmaceutics ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 1132
Author(s):  
Antonella Obinu ◽  
Elena Piera Porcu ◽  
Sandra Piras ◽  
Roberta Ibba ◽  
Antonio Carta ◽  
...  

The role of mycobacterial efflux pumps in drug-resistant tuberculosis has been widely reported. Recently, a new compound, named SS13, has been synthesized, and its activity as a potential efflux inhibitor has been demonstrated. In this work, the chemical–physical properties of the SS13 were investigated; furthermore, a formulative study aimed to develop a formulation suitable for oral administration was performed. SS13 shows nonintrinsic antitubercular activity, but it increases the antitubercular activity of all the tested drugs on several strains. SS13 is insoluble in different simulated gastrointestinal media; thus, its oral absorption could be limited. Solid lipid nanoparticles (SLNs) were, therefore, developed by using two different lipids, Witepsol and/or Gelucire. Nanoparticles, having a particle size (range of 200–450 nm with regards to the formulation composition) suitable for intestinal absorption, are able to load SS13 and to improve its permeation through the intestinal mucosa compared to the pure compound. The cytotoxicity is influenced by the concentration of nanoparticles administered. These promising results support the potential application of these nanocarriers for increasing the oral permeation of SS13 in multidrug-resistant tuberculosis management.

Author(s):  
Narendar Dudhipala

In the recent scenario, lipid nanoparticles gain much attention on the oral absorption of drugs to enhance therapeutic effectiveness after oral administration. Pharmacodynamic activity of drug mainly describes the pharmacological and therapeutic activity of drug to the biological system. Lipid nanoparticles especially solid lipid nanoparticles are made of physiological inert lipid molecules and promotes the lymphatic transport. Abundant literature is available on the effect of lipid nanoparticles and other colloidal carrier systems on the pharmacokinetic parameters of poorly bioavailable drugs, to improve their oral absorption and also respective mechanisms for the improved oral bioavailability. However, little literature is reported on the pharmacodynamic activity and the effect of dose on the pharmacodynamic activity. It is of paramount importance to assess the influence of lipid nanoparticles on pharmacotherapeutic actions of specific drug classes. Therefore, current review is mainly focused on the role of solid lipid nanoparticles on the pharmacodynamic action and advantages of the developed delivery systems with respect to pharmacodynamic activity.    


2005 ◽  
Vol 13 (2) ◽  
pp. 172-174 ◽  
Author(s):  
Rishen Naidoo ◽  
Anu Reddi

The emergence of multidrug-resistant tuberculosis poses a serious challenge to traditional drug therapy. In view of the relapse rate of up to 50% following medical management, there has been renewed interest in the role of surgery for this problem. We report our experience with lung resection for this condition. Over a 5-year period, resection was performed in 23 patients who were diagnosed with multidrug resistance after completing a course of standard chemotherapy and at least 3 months of second-line therapy. Pneumonectomy was performed in 17 patients and lobectomy in 6. There was no operative or postoperative mortality. Major complications developed in 4 patients (17.4%): 2 had post-pneumonectomy empyema and 2 underwent rethoracotomy for bleeding. Ten patients were sputum positive preoperatively, and only 1 remained positive after surgery. The patients were put on appropriate chemotherapy and followed up for 18 months. The cure rate was 95.6%. Pulmonary resection can be considered as an important adjunct to medical therapy in carefully selected patients: those who have localized disease with adequate pulmonary reserve, or who have multiple previous relapses, or whose sputum remains positive after 4 to 6 months of appropriate medical treatment. Surgery offers high cure rates with acceptable morbidity and mortality.


2020 ◽  
Vol 11 (13) ◽  
pp. 1985-1995 ◽  
Author(s):  
Ruiqi Huang ◽  
Yanjing Zhu ◽  
Lijuan Lin ◽  
Simin Song ◽  
Liming Cheng ◽  
...  

2014 ◽  
Vol 31 (8) ◽  
pp. 1978-1988 ◽  
Author(s):  
Tuan Hiep Tran ◽  
Thiruganesh Ramasamy ◽  
Duy Hieu Truong ◽  
Beom Soo Shin ◽  
Han-Gon Choi ◽  
...  

2015 ◽  
Vol 61 (6) ◽  
pp. 1029-1030 ◽  
Author(s):  
Abed Zahedi Bialvaei ◽  
Hossein Samadi Kafil ◽  
Mohammad Asgharzadeh

2021 ◽  
Vol 11 (2) ◽  
pp. 204-208
Author(s):  
D Raju

Solid lipid nanoparticles (SLNs) considered as an alternative vehicle for the enhanced oral absorption of drugs, and also to enhance therapeutic effectiveness after oral administration. Pharmacodynamic activity of drug is mainly describes the pharmacological and therapeutic activity of drug to the biological system. Lipid nanoparticles especially SLNs made of physiological inert lipid molecules and helps the lymphatic transport. Numerous literatures is available on the effect of SLNs and other colloidal carrier systems on the pharmacokinetic activity of poorly bioavailable drugs, to improve their oral absorption and also respective mechanisms for the improved oral bioavailability. However, very few literatures is reported on the pharmacodynamic activity and the effect of dose on the pharmacodynamic activity. Therefore, the current review is mainly dealing with the effect of SLNs on the pharmacodynamic activity discussed.   Keywords: Oral absorption, solid lipid nanoparticles, lymphatic transport, pharmacokinetics, pharmacodynamics.


2017 ◽  
Vol 8 (3) ◽  
pp. 11 ◽  
Author(s):  
Sean O'Brien ◽  
Jacy Downey

Objectives: The primary objective is to investigate the public’s perception about the role of the community pharmacist in Peru’s directly observed treatment, short course (DOTS) program. The secondary objective is to assess perceived barriers that would prevent the public from utilizing community pharmacists in order to identify future opportunities for community pharmacists to increase adherence to multidrug-resistant tuberculosis (MDR-TB) therapy. Design: Qualitative study comprised of an 8 close-ended survey questionnaire. Setting: Healthcare clinics established by a medical mission group in Lima and surrounding communities, Peru, from July 13 to July 27, 2015. Participants: Patients 15 years of age and over who sought healthcare at the clinics. Main outcome measures: Public’s perception about the role of the community pharmacist in Peru and barriers that would prevent the public from seeking a community pharmacist. Results: Out of the 445 patients approached, 438 patients completed the survey, resulting in a 98% response rate. More than half (52%) of the respondents were likely to seek a community pharmacist to assist them in completing a MDR-TB medication regimen. Almost half (48%) of the respondents felt comfortable with assistance of a community pharmacist in completing an MDR-TB regimen. The physician was the first health care professional that was contacted for all medical situations, including drug-related questions (61%). Lack of privacy in the pharmacy (53%) and busyness of the pharmacists (52%) were the top perceived barriers for asking community pharmacists questions. Conclusion: This study highlights the need for pharmacist participation in Peru’s DOTS program. Furthermore, this investigation has identified several issues of concern related to current community pharmacy practice in Peru. Therefore, future efforts may be necessary to address these identified areas of opportunity to promote the community pharmacist’s role in health screening, drug therapy monitoring, and counseling to decrease the public health burden of MDR-TB. Conflict of Interest We declare no conflicts of interest or financial interests that the authors or members of their immediate families have in any product or service discussed in the manuscript, including grants (pending or received), employment, gifts, stock holdings or options, honoraria, consultancies, expert testimony, patents or royalties.   Type: Original Research


2016 ◽  
Vol 6 (3) ◽  
pp. 27-27
Author(s):  
Hayrettin EROĞLU ◽  
Ayşe YENİLMEZ ◽  
Arif Kursad AYAN ◽  
Cemal GÜNDOĞDU ◽  
Sare ŞİPAL

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