Drug loaded liposomes of mesalamine incorporated into disease responsive microgels (Micro) for treating allergic asthma: An approach using smart drug delivery system

Raju, Rama Satyanarayana; Kumar, Monu; Elango, K; Ambhore, Nilesh Sudhakar; Mulukutla, Shashank; Kuppusamy, Gowthamarajan

doi:10.1183/13993003.congress-2015.pa5011

Cited by 3 publications

(2 citation statements)

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“…The pathophysiology of asthma manifests as a result of various factors such as genetic, environmental, lifestyle associated, and more importantly endogenous physiological conditions (2,13,24,25,(53)(54)(55). In the quest for identifying the underlying endogenous factors contributing to the observed gender differences in the prevalence and severity of asthma, multiple research groups including our own have explored the role of sex-steroids and their receptors in asthma, especially estrogen (13,17,25,(56)(57)(58) and ER's (19,20,22,23), with very little information on androgens (27,34,43,59,60) and AR (30,35,39,41).…”

Section: Discussionmentioning

confidence: 99%

Androgen receptor activation alleviates airway hyperresponsiveness, inflammation, and remodeling in a murine model of asthma

Kalidhindi

Ambhore

Balraj

et al. 2021

American Journal of Physiology-Lung Cellular and Molecular Phys

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Epidemiological studies demonstrate an apparent sex-based difference in the prevalence of asthma, with a higher risk in boys than girls, which is reversed post-puberty, where women become more prone to asthma than men, suggesting a plausible beneficial role for male hormones, especially androgens as a regulator of pathophysiology in asthmatic lungs. Using a murine model of asthma developed with mixed allergen (MA) challenge, we report a significant change in airway hyperresponsiveness (AHR), as demonstrated by increased thickness of epithelial and airway smooth muscle layers and collagen deposition, as well as Th2/Th17 biased inflammation in the airways of non-gonadectomized (non-GDX) and gonadectomized (GDX) male mice. Here, compared to non-GDX mice, MA induced AHR and inflammatory changes were more prominent in GDX mice. Activation of androgen receptor (AR) using 5α-Dihydrotestosterone (5a-DHT, AR agonist) resulted in decreased Th2/Th17 inflammation and remodeling associated changes, resulting in improved lung function compared to MA alone challenged mice, especially in GDX mice. These changes were not observed with Flutamide (Flut, AR antagonist). Overall, we show that AR exerts a significant and beneficial role in asthma by regulating AHR and inflammation.

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Section: Discussionmentioning

confidence: 99%

Androgen receptor activation alleviates airway hyperresponsiveness, inflammation, and remodeling in a murine model of asthma

Kalidhindi

Ambhore

Balraj

et al. 2021

American Journal of Physiology-Lung Cellular and Molecular Phys

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“…Fifty-four Wistar rats were randomly assigned into nine groups of six animals in each group. The liposomal formulation of conessine [31][32][33] and pure conessine were dissolved in Tris KCl buffer (pH 7.4) and then orally administered to rats at a dose equivalent of 20 mg/kg. Aliquots of approximately 0.5 ml of blood samples were collected via cardiac puncture at time intervals of 0 min (predose), 0.5, 1.0, 1.5, 2.0, 4.0, 6.0, 8.0 and 12 h post-dose.…”

Section: Pharmacokinetics and Tissue Distribution Studymentioning

confidence: 99%

Determination of Histamine H3-Receptor Antagonist Conessine in Wistar Rat Plasma by a Rapid and Sensitive RP-UFLC Method: Application to a Pharmacokinetic Study

Ambhore¹,

Kalidhindi²,

Mohire³

et al. 2020

JYP

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Objectives: Epidemiological data suggests the highest density of histamine H3-receptors (H3R) in basal ganglia of central nervous system (CNS) wherein they function as inhibitory auto-receptors and control the release of many neurotransmitters. Inhibition of H3R increases the turnover of neurotransmitters, especially dopamine in basal ganglia and could be beneficial to treat Parkinson's disease. Methods: In this study, we formulated the brain targeting liposomes of conessine, a selective antagonist for H3R to increase bioavailability and developed and validated a rapid and sensitive reverse phase ultra-force liquid chromatographic (RP-UFLC) method and to quantitate conessine in Wistar rat plasma and tissue. Plasma and tissue samples were extracted by protein precipitation technique using acetonitrile (ACN) and aripiprazole as the internal standard. Chromatographic separation was performed on the Hibar C 18 column with a mobile phase of Hexane Sulphonic acid (10 mM, pH 10.0 adjusted with ammonia) and methanol at a flow rate of 0.9 ml/min. Results: The lower limit of quantification of the developed method was 4.0 ng/ml and 6.0 ng/g in plasma and tissue samples, respectively. Liposomes of conessine (equivalent to 20 mg/kg) administered orally to animals, demonstrated remarkable absorption into the systemic circulation with maximum concentration (~8700 ng/ ml) within 2.0 h. The order of area under curve was found to be kidney> brain> liver> lungs> spleen> heart. Conclusion: The liposomes of conessine were rapidly taken up into the brain and showed a good brain concentration after 2.0 h; sustenance up to 4.0 h was achieved which is better than conessine solution.

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Sex-Steroid Signaling in Lung Diseases and Inflammation

Ambhore

Kalidhindi

Sathish

2021

Advances in Experimental Medicine and Biology

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Drug loaded liposomes of mesalamine incorporated into disease responsive microgels (Micro) for treating allergic asthma: An approach using smart drug delivery system

Cited by 3 publications

References 0 publications

Androgen receptor activation alleviates airway hyperresponsiveness, inflammation, and remodeling in a murine model of asthma

Androgen receptor activation alleviates airway hyperresponsiveness, inflammation, and remodeling in a murine model of asthma

Determination of Histamine H3-Receptor Antagonist Conessine in Wistar Rat Plasma by a Rapid and Sensitive RP-UFLC Method: Application to a Pharmacokinetic Study

Sex-Steroid Signaling in Lung Diseases and Inflammation

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