Physicochemical Characterizations and Pharmacokinetic Evaluation of Pentazocine Solid Lipid Nanoparticles against Inflammatory Pain Model
Zaheer Ullah Khan,Anam Razzaq,Najeeb Ur Rehman,Hira Khan,Taous Khan,Ashraf A. Khan,Norah A. Althobaiti,Farid Menaa,Haroon Iqbal,Naveed Ullah Khan +9 more
Reads0
Chats0
TLDR
Results demonstrated that PTZ-loaded SLNs can improve the bioavailability of PTZ by bypassing the hepatic metabolism via the lymphatic uptake, for controlled and sustained drug delivery.Abstract:
Pentazocine (PTZ), a narcotic-antagonist analgesic, has been extensively used in the treatment of initial carcinogenic or postoperative pain. Hepatic first-pass metabolism results in low oral bioavailability and high dose wastage. Herein, 10 mg (-)-Pentazocine (HPLC-grade) was incorporated to solid lipid nanoparticles (SLNs) using a double water-oil-water (w/o/w) emulsion by solvent emulsification–evaporation technique, followed by high shear homogenization to augment its oral bioavailability, considering the lymphatic uptake. The resulting SLNs were characterized for zeta potential (ZP), particle size (PS), and polydispersity index (PDI) using a zetasizer. The entrapment efficiency (EE) and loading capacity (LC) were calculated. Chemical interactions, through the identification of active functional groups, were assessed by Fourier-transformed infrared (FTIR) spectroscopy. The nature (crystallinity) of the SLNs was determined by X-ray diffractometry (XRD). The surface morphology was depicted by transmission electron microscopy (TEM). In vitro (in Caco-2 cells) and in vivo (in male Wistar rats) investigations were carried out to evaluate the PTZ release behavior and stability, as well as the cellular permeation, cytotoxicity, systemic pharmacokinetics, antinociceptive, anti-inflammatory, and antioxidative activities of PTZ-loaded SLNs, mainly compared to free PTZ (marketed conventional dosage form). The optimized PTZ-loaded SLN2 showed significantly higher in vitro cellular permeation and negligible cytotoxicity. The in vivo bioavailability and pharmacokinetics parameters (t1/2, Cmax) of the PTZ-loaded SLNs were also significantly improved, and the nociception and inflammation, following carrageenan-induced inflammatory pain, were markedly reduced. Concordantly, PTZ-loaded SLNs showed drastic reduction in the oxidative stress (e.g., malonaldehyde (MDA)) and proinflammatory cytokines (e.g., Interleukin (IL)-1β, -6, and TNF-α). The histological features of the paw tissue following, carrageenan-induced inflammation, were significantly improved. Taken together, the results demonstrated that PTZ-loaded SLNs can improve the bioavailability of PTZ by bypassing the hepatic metabolism via the lymphatic uptake, for controlled and sustained drug delivery.read more
Citations
More filters
Journal ArticleDOI
Fabrication of Ethosomes Containing Tocopherol Acetate to Enhance Transdermal Permeation: In Vitro and Ex Vivo Characterizations
Naveed Akhtar,Naveed Akhtar,Farid Menaa,Walaa Alharbi,Fatima S. Alaryani,Alia Musfer Alqahtani,Faizan Ahmad +6 more
TL;DR: In this article , a cold method technique was used to produce the ethosomes and an in vitro evaluation of viscosity, conductivity, and pH stability was carried out for three months.
Journal ArticleDOI
Fabrication and Characterizations of Pharmaceutical Emulgel Co-Loaded with Naproxen-Eugenol for Improved Analgesic and Anti-Inflammatory Effects
Barkat Ali Khan,Sajeel Ahmad,Muhammad Khalid Khan,Khaled M. Hosny,Deena Bukhary,Haroon Iqbal,Samar S.A. Murshid,Abdulrahman A. Halwani,Mohammed Alissa,Farid Menaa +9 more
TL;DR: It was concluded that transdermal delivery of naproxen-eugenol emulgel synergized the anti-inflammatory and analgesic effects of napoxen and eugenol.
Journal ArticleDOI
Lipid nanoparticles for delivery of RNA therapeutics: Current status and the role of in vivo imaging
TL;DR: In this article , the authors provide a thorough introduction and explanation of the components of LNPs and its functions along with various production methods of formulating LNs and explore recent advances in LNP-based RNA therapeutics in clinics and clinical trials.
Journal ArticleDOI
Synthesis and In Vitro/Ex Vivo Characterizations of Ceftriaxone-Loaded Sodium Alginate/poly(vinyl alcohol) Clay Reinforced Nanocomposites: Possible Applications in Wound Healing
Shabana Bibi,Sadullah Mir,Wajid Rehman,Farid Menaa,Alia Gul,Fatima S. Alaryani,Ali Alqahtani,Sirajul Haq,Magda H. Abdellatif +8 more
TL;DR: In this paper , the in vitro properties of the antibiotic ceftriaxone sodium (CTX) once encapsulated into sodium alginate (SA)/poly(vinyl alcohol)PVA-clay reinforced nanocomposite films were investigated.
Journal ArticleDOI
In Vitro and Ex Vivo Evaluation of Mangifera indica L. Extract-Loaded Green Nanoparticles in Topical Emulsion against Oxidative Stress and Aging
TL;DR: In this paper , Mangifera indica extract was loaded into nanolipid carriers (M-NLCs) to create a green topical formulation that would boost antiaging efficacy and address penetration deficit.
References
More filters
Journal ArticleDOI
Solid lipid nanoparticles: Production, characterization and applications
W. Mehnert,Karsten Mäder +1 more
TL;DR: An overview about the selection of the ingredients, different ways of SLN production and SLN applications, and the in vivo fate of the carrier are presented.
Journal ArticleDOI
Role of proinflammatory cytokines in the pathophysiology of osteoarthritis
TL;DR: The current knowledge regarding the role of proinflammatory cytokines in the pathophysiology of OA is discussed and the potential of anticytokine therapy in the treatment of this disease is addressed.
Journal ArticleDOI
The production and characteristics of solid lipid nanoparticles (SLNs)
TL;DR: It seemed this modified method could prepare high quality SLNs loading lipophilic drugs, and it was suggested that the majority of the SLNs were less ordered arrangement of crystals, and this was favorable for increasing the drug loading capacity.
Journal ArticleDOI
A brief review on solid lipid nanoparticles: part and parcel of contemporary drug delivery systems
Yongtao Duan,Abhishek Dhar,Chetan K. Patel,Mehul Khimani,Swarnali Neogi,Prolay Sharma,Nadavala Siva Kumar,Rohit L. Vekariya +7 more
TL;DR: Although nano-structured lipid carriers and SLNs are based on lipids and surfactants, the effect of these two matrixes to build excipients is also discussed together with their pharmacological significance with novel theranostic approaches, stability and storage.
Related Papers (5)
Selection of drug candidates for gastroretentive dosage forms: pharmacokinetics following continuous intragastric mode of administration in a rat model.
Leonid Kagan,Amnon Hoffman +1 more