In Vitro-In Vivo Evaluation of Novel Co-spray Dried Rifampicin Phospholipid Lipospheres for Oral Delivery

Singh, Charan; Koduri, L.V. Seshu Kumar; Bhatt, Tara Datt; Jhamb, Sarbjit Singh; Mishra, Vijay; Gill, Manjinder Singh; Suresh, Sarasija

doi:10.1208/s12249-016-0491-5

Cited by 18 publications

(4 citation statements)

References 33 publications

(34 reference statements)

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“…Some studies revealed that MMAD of 1-5µm could be optimal range particles size for pulmonary delivery [48]. In our study, obtained results suggested that developed PLGA composites showed an acceptable range of MMAD (2.50 ± 0.20 nm), GSD (65.50 ± 5.50%), and (92.28 ± 0.2%) as shown in Table 3, signifying an e cient for drug delivery [49,50]. Moreover, the drug deposition study performed by Next Generation Impactor (NGI) showed the highest deposition for NAC-PLGA@Cs as compared to NAC-PLGA NPs at stage 3 followed by 4 and 5indicating the deep lung deposition of developed inhalable composites as shown in Fig.…”

Section: In Vitro Pulmonary Deposition Studysupporting

confidence: 56%

Inhalable N-Acetylcysteine loaded PLGA composites for Tuberculosis: In Vitro Aersolization and Efficacy Studies

Chaudhary

Puri

Singh

et al. 2023

Preprint

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N-Acetylcysteine (NAC) is a precursor of Glutathione (GSH) which possess an immense potential of mucolytic, anti-inflammatory and antioxidant properties against several diseases including tuberculosis. Since last several decades, NAC is being primarily used to treat lung conditions as well as paracetamol-induced liver toxicity However, NAC exhibited potential antimycobacterial activity through several mechanism including immunomodulation, enhancement of GSH level, and by direct antimycobacterial effect. Herein, we synthesized and characterized lactose coated N-acetylcysteine loaded PLGA composites (NAC-PLGA@Cs) by double emulsion solvent evaporation technique. The physicochemical characterization studies revealed the compatibility of the drug with excipients. Moreover, NAC-PLGA@Cs showed particle size with 310 ± 5.5nm, PDI with 0.15 ± 0.1, and zeta potential with − 11.5 ± 0.4 mV. In vitro release study suggested the biphasic release profile. Likewise, in vitro lung deposition studies revealed remarkable lung deposition parameters, indicating effective particles size for efficient pulmonary delivery. Additionally, in vitro study for antimycobacterial activity exhibited superior antibacterial activity against MTB H37Rv. Subsequently, we hypothesized that NAC incorporated PLGA composites could be a novel approach in the battle of fighting for pulmonary tuberculosis.

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Section: In Vitro Pulmonary Deposition Studysupporting

confidence: 56%

Inhalable N-Acetylcysteine loaded PLGA composites for Tuberculosis: In Vitro Aersolization and Efficacy Studies

Chaudhary

Puri

Singh

et al. 2023

Preprint

Self Cite

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“…Those bacteria may spread, if they are alive, through the lymphatic system or the circulation to the regional lymph nodes, the apex of the lung, kidneys, brain, and bony parts of the body, where TB sickness is most likely to develop. This process of dissemination sets the immune system for an expanded response (Figure 1D) [27]. To use an analogy, a bacterial jail called a granuloma aims to isolate a bacterium beneath an enclosure of immune cells.…”

Section: Tb Pathophysiologymentioning

confidence: 99%

Nanocarriers in Tuberculosis Treatment: Challenges and Delivery Strategies

Kumar,

Virmani,

Kumar

et al. 2023

Pharmaceuticals

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The World Health Organization identifies tuberculosis (TB), caused by Mycobacterium tuberculosis, as a leading infectious killer. Although conventional treatments for TB exist, they come with challenges such as a heavy pill regimen, prolonged treatment duration, and a strict schedule, leading to multidrug-resistant (MDR) and extensively drug-resistant (XDR) strains. The rise of MDR strains endangers future TB control. Despite these concerns, the hunt for an efficient treatment continues. One breakthrough has been the use of nanotechnology in medicines, presenting a novel approach for TB treatment. Nanocarriers, such as lipid nanoparticles, nanosuspensions, liposomes, and polymeric micelles, facilitate targeted delivery of anti-TB drugs. The benefits of nanocarriers include reduced drug doses, fewer side effects, improved drug solubility, better bioavailability, and improved patient compliance, speeding up recovery. Additionally, nanocarriers can be made even more targeted by linking them with ligands such as mannose or hyaluronic acid. This review explores these innovative TB treatments, including studies on nanocarriers containing anti-TB drugs and related patents.

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“…In another study novel cospray dried RMP phospholipid lipospheres (SDRPL) to influence on RMP solubility and oral BA. [39] Solid-state techniques were employed to characterize the liposphere formulation. SDRPL solubility was determined in distilled water.…”

Section: Rifampicin (Rmp)mentioning

confidence: 99%

Untitled

Patra¹

2018

AJP

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Solid lipid-based drug delivery systems such as lipospheres, solid lipid nanoparticles, and nanostructured lipid carriers have high stability, high carrier capacity, feasibility of incorporation of both hydrophilic and hydrophobic substances, and feasibility of variable routes of administration, including oral, topical, and parenteral and pulmonary routes. Highly lipophilic and poorly water-soluble compounds that also undergo extensive presystemic intestinal metabolism are the ultimate candidates for incorporation into solid lipid-based drug delivery systems to obtain increased and less variable bioavailability (BA). Increase in biliary and pancreatic secretions, stimulation of lymphatic transport, improvement of intestinal wall permeability, reduction of metabolism and efflux activity, and alteration in mesenteric and liver blood flow, which appreciably contribute to improved oral BA of the drug.

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In Vitro-In Vivo Evaluation of Novel Co-spray Dried Rifampicin Phospholipid Lipospheres for Oral Delivery

Cited by 18 publications

References 33 publications

Inhalable N-Acetylcysteine loaded PLGA composites for Tuberculosis: In Vitro Aersolization and Efficacy Studies

Inhalable N-Acetylcysteine loaded PLGA composites for Tuberculosis: In Vitro Aersolization and Efficacy Studies

Nanocarriers in Tuberculosis Treatment: Challenges and Delivery Strategies

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