Design and development of nasal mucoadhesive microspheres containing tramadol HCl for CNS targeting

Belgamwar, Veena S.; Patel, Hitesh S; Joshi, Ashwini S.; Agrawal, Anshuman; Surana, Sanjay J.; Tekade, Avinash R.

doi:10.3109/10717544.2011.557787

Cited by 37 publications

(19 citation statements)

References 18 publications

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“…However, X-ray diffraction pattern of LT loaded CH microspheres did not show any peaks suggesting that the LT might have been molecularly dispersed in the CH or converted in amorphous form in CH microspheres. [36] The results are also in accordance with the DSC analysis of LT CH microsphere. …”

Section: X-ray Diffraction Studiessupporting

confidence: 78%

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Taksande¹

2017

AJP

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Aim: Due to the presence of rich blood circulation and non-invasive nature of administration, the nasal route has been established as valuable therapeutic alternatives. This study was designed with the basic objective to formulate mucoadhesive microspheres of anticonvulsant drug, lamotrigine (LT) for intranasal delivery and to carry out its pharmacodynamic investigations to benefit the emergency cases of epileptic seizures. Materials and Methods:The microspheres were prepared by ionotropic gelation method and characterized for morphology scanning electron microscopy, particle size, drug entrapment efficiency, thermal behavior (differential scanning calorimetry), and crystallinity (X-ray diffraction), in vitro swelling studies, in vitro drug diffusion, ex vivo bioadhesion, and ex vivo biocompatibility studies in excised sheep nasal mucosa. The resultant LT loaded chitosan (CH) microspheres were further evaluated for pharmacodynamic efficacy in pentylenetetrazol (PTZ) induced seizures in mice. Result and Discussion: Results demonstrated that the microspheres were discrete, smooth, and spherical in shape with size 24.5 ± 2.62 to 48.52 ± 2.34 µm, appropriate for nasal drug delivery. The CH-based nasal LT microspheres demonstrated high encapsulation efficacy, strong bioadhesion potential, and high permeation without any signs of morphological toxicity in excised sheep nasal mucosa. Importantly the intranasal administration of LT microspheres delayed the onset of clonic convulsion and offered complete protection against the PTZ induced seizures in mice compared to its peripheral administration. Conclusion: Thus, the formulation of LT loaded CH mucoadhesive microspheres offers promising advantages over conventional dosage with its immediate onset of action.

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Section: X-ray Diffraction Studiessupporting

confidence: 78%

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Taksande¹

2017

AJP

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“…The diameters were determined using a suitable objective (10X, 40X, 100X). The average particle size of nanoparticles can be given by the following formula [22].…”

Section: Characterization Of Nanoparticles Particle Size and Zeta Potmentioning

confidence: 99%

Intranasal Topiramate Polymeric Nanoparticles for Epilepsy: In Vitro and Ex-Vivo Investigation

et al. 2020

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Objective: The presence of tight junctions in blood-brain barrier creates a major problem for the delivery of drugs and severely affects adequate therapeutic concentration to reach the brain. For the treatment of epilepsy, oral route of administration is most convenient but shows delayed absorption. Moreover, in emergency cases, parenteral administration is not possible as it requires medical assistance. Thus, an alternative route of drug delivery is highly desirable for an effective outcome. Methods: In the present study, bioadhesive chitosan nanoparticles of topiramate for intranasal administration were prepared by ionotropic gelation method using chitosan as bioadhesive polymer and sodium tripolyphosphate as the crosslinking agent. The prepared nanoparticles were evaluated for physicochemical properties like particle size, surface morphology, drug content, entrapment efficiency, thermal behavior and crystallinity, in vitro drug diffusion, ex vivo bio adhesion, and ex vivo biocompatibility studies in excised sheep nasal mucosa. Results: Differential scanning calorimetry and x-ray diffraction study showed molecular dispersion of drug into the polymer matrices and conversion of it into an amorphous form. Nanoparticles obtained were discrete in nature (size 313.5 nm) and appropriate for intranasal administration. The topiramate nanoparticles revealed high encapsulation efficacy, strong bioadhesion potential and high ex vivo permeation and did not exhibit any deformity to the nasal mucosa. In vitro drug diffusion of optimized formulation showed 92.91% release of drugs after 180 min. Ex-vivo permeation of drugs across nasal mucosa was 89.03 % after 180 min. Conclusion: Hence, the intranasal administration of topiramate using chitosan can be a promising alternative for brain targeting and the treatment of epilepsy.

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“…Theoretical yield is the total weight of the raw materials used for preparation, whereas practical yield represents the weight of the microsphere, which was practically obtained (Belgamwar et al, 2011).…”

Section: Percentage Yieldmentioning

confidence: 99%

Polymeric Microsphere Formulation for Colon Targeted Delivery of 5-Fluorouracil Using Biocompatible Natural Gum Katira

Karan

Choudhury

Chakra

et al. 2019

Asian Pac J Cancer Prev

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Controlled release delivery system of chemotherapeutic agents at the site of colon endorses modern drug-entrapped delivery tools, which release the entrappedagents at a controlled rate for anextended period providing patient compliance and additional protection from the degradinggastric environment. Thus, the present study was aimed to develop and optimize a novel polymeric microsphere of 5-fluorouracil (5-FU) using natural gum katira to obtain an optimal therapeutic response at the colon. Due course of experimentation, in-vivo safety profile of the gum katira in an animal model was established. Modified solvent extraction/evaporation technique wasemployed to encapsulate 5-FU in the natural polymeric microsphere and was characterized using in-vitro studies to investigate particle size, morphology, encapsulation efficiency and release of the drug from developed formulation. Formulated and optimized polymeric microsphere of 5-FU using gum katira polymer own optimal physicochemical characteristics with a fine spherical particle with size ranged from 210.37±7.50 to 314.45±7.80 µm.Targeted microsphere exhibited good cytotoxicity and also has high drug entrapment efficiency, and satisfactory release pattern of the drug within a time frame of 12 h. Finally, we foresee that the optimized polymeric gum katiramicrosphere of 5-FU could be a promising micro-carrier for efficient colon drug targeting delivery tool with improved chemotherapeutic efficacy against colon cancer.

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Design and development of nasal mucoadhesive microspheres containing tramadol HCl for CNS targeting

Cited by 37 publications

References 18 publications

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Intranasal Topiramate Polymeric Nanoparticles for Epilepsy: In Vitro and Ex-Vivo Investigation

Polymeric Microsphere Formulation for Colon Targeted Delivery of 5-Fluorouracil Using Biocompatible Natural Gum Katira

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