Formulation, Development, and Evaluation of Floating Pulsatile Drug Delivery System of Atenolol

Jagdale, Swati; Sali, Monali S.; Barhate, Ajay L.; Kuchekar, Bhanudas S.; Chabukswar, Anuruddha R.

doi:10.5731/pdajpst.2013.00916

Cited by 12 publications

(5 citation statements)

References 27 publications

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“…This equation describes the relative significance of Fickian (n ≤ 0.5) and Case II (n ≤ 1.0) transport in anomalous diffusion. Kinetic studies were performed by adjusting the release profiles to Higuchi, first-order and zero-order kinetics equations 55 . pharmacological study.…”

Section: Formulation Of Medicated Mn Arraysmentioning

confidence: 99%

Characterization and Pharmacological Evaluation of Anti-Cellulite Herbal Product(s) Encapsulated in 3D-Fabricated Polymeric Microneedles

Amer

Elosaily

Bakr

et al. 2020

Sci Rep

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Skin health is vital for a healthy body. Herbal remedies have long been used for skin care, and their global use has tremendously increased over the past three decades. Although cellulite is seen as a normal condition by the medical community, it is considered a serious cosmetic concern for most affected women. Many topical anti-cellulite creams are available on the market, but unfortunately, their efficacy has not been proven scientifically. Microneedles (MNs) represent a new approach to enhance the permeation of loaded medication through the skin. In this study, the anti-cellulite effects of Vitex agnus-castus and Tamarindus indica extracts were compared using safe and effective polymeric MNs. This delivery system offers a painless alternative to the combined treatment strategy of microneedling devices and anti-cellulite products. The selected standardized extracts were evaluated for their mineral, phenolic and flavonoid contents, which are correlated to a promising antioxidant effect, as demonstrated by an in vitro radical scavenging activity assay. 3D-printing techniques were chosen for fabrication of a micromold, which is inexpensive for mass production. To ensure that MNs were sufficiently strong to perforate the skin without breaking, axial failure force was measured using a micro-mechanical test machine. The anticellulite effects of MNs were assessed using an in vivo dietinduced obesity guinea pig model. Skin properties, histopathology and inflammatory markers were examined. MNs loaded with plant extracts were statistically comparable in normalizing the oxidative state and reducing inflammation, while myeloperoxidase levels were more significantly reduced by T. indica than by V. agnus-castus. This novel delivery system opens the door for new transdermal strategies for cellulite management. The skin is a chief barrier that provides protection for the human body. The outermost layer of the epidermis (stratum corneum, SC) is mainly responsible for this barrier property. Cellulite is a skin condition that affects up to 90% of women over 20 years of age and only 2% of men. It includes changes in skin appearance, with an orange-peel-like texture (mostly on the hips and buttocks) due to the expansion of fat lobules out of their connective frame and into the dermis 1-3. Cellulite is a pathologically complicated condition that is associated with decreased microcirculation, oedema, overgrowth of adipocytes, oxidative stress, continuous inflammation, and changes in the extracellular matrix 4,5. Some pharmaceutical products can treat cellulite by increasing the microvascular flow, inducing lipolysis, restoring dermis and connective tissue structures, and preventing

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Section: Formulation Of Medicated Mn Arraysmentioning

confidence: 99%

Characterization and Pharmacological Evaluation of Anti-Cellulite Herbal Product(s) Encapsulated in 3D-Fabricated Polymeric Microneedles

Amer

Elosaily

Bakr

et al. 2020

Sci Rep

View full text Add to dashboard Cite

show abstract

“…Press coating was used to create a unique colon-focused tablet formulation, which is a quickly dissolving tablet of atenolol with guar gum and Eudragit L-100 as a barrier layer. Different polymer ratios were used to provide an appropriate lag time for the treatment of angina pectoris [34]. Patil created a chrono-regulated pulsatile drug delivery system for captopril, which is used to treat cardiovascular disease (hypertension).…”

Section: The Cardiovascular Systemmentioning

confidence: 99%

Pulsatile Drug Delivery: A Strategy for Treating Chronotherapeutic Ailments

J.,

B.,

M. F.

2023

Int J Curr Pharm Sci

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Modern drug delivery systems have been promoted to a unique notion of chronopharmacology, i.e., the ability to provide the medicament to a patient in a staggered profile, as the discipline of chronobiology has advanced. The main disadvantage of developing such a delivery system that fits the circadian cycle is the lack of accurate technology (Pulsatile drug delivery system, PDDS). Pulsatile devices are gaining popularity because they deliver the medicine to the correct region of action at the correct time, allowing for spatial and temporal dosing and compliance among patients. These technologies are meant to work with the body's natural circadian cycle. The circadian rhythm affects various biological systems in humans, including metabolism, physiology, behaviour, sleep patterns, hormone synthesis, and so on. This article addresses several methods, such as osmotic systems, capsular systems, single and multiple-unit programable devices that rely on soluble or erodible polymer coatings, and the usage of rupturable membranes. The present review covered the rationale for the creation of pulsatile drug delivery systems, benefits, limitations the types of diseases that require pulsatile release, categorization, and assessments of pulsatile system of drug delivery.

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“…The value of n for formulations OF-1 to OF-9 was in the range of 0.48-0.60 which indicates the drug transport mechanism to be anomalous transport (n = 0.45-0.89). [28] Characterization study by FTIR spectroscopy FTIR spectrophotometry was carried out for identification and affinity of formulation composition. The FT-IR spectra of ketorolac tromethamine show O-H stretching at 2916 cm -1 , N-H stretching at 3345 cm -1 , aromatic C-H stretching at 2848 cm -1 , C=O stretching at 1651 cm -1 , while C=C and C-N stretching show at 1579 and 1244 cm -1 , respectively.…”

Section: Simentioning

confidence: 99%

Untitled

2023

AJP

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Introduction:The primary objective of this research work was to design a hydrodynamically balanced system (HBS) of ketorolac tromethamine based on the combination of swelling and effervescence mechanism that would result in minimum floating lag time (FLT), remain buoyant for extended period, and sustain the drug release for 12 h. Materials and Methods: HBS tablets of ketorolac tromethamine were prepared by wet granulation method using 3 2 full factorial design, where amount of hydroxypropyl methylcellulose K4M (X 1 ) and sodium bicarbonate (NaHCO 3 ) (X 2 ) was taken as independent variables. The responses studied were Y 1 (hardness), Y 2 (FLT), Y 3 total floating time (TFT), Y 4 (swelling index [SI] in pH1.2), and Y 5 (t 80%) by plotting response surface graph and contour plots. Results: The FLT of prepared batches was in the range of 35.24 ± 0.04-116 ± 0.06 s and the minimum FLT was shown by OF-9 (35.24 s) batch. The TFT of all batches showed buoyancy and intactness for 24 h. The swelling in pH 1.2 at 8 h ranged between 47.80 ± 0.89 and 54.33 ± 0.11 with a significant difference (P < 0.0001). In vitro drug release study revealed that more than 95% of drug was released in 12 h and OB-2 showed 10 h to release 80% of the drug. The analytical characterization revealed the compatibility of drug with excipient and polymers. The stability studies performed for 6 months for OF-7 and OF-8 batches showed no change in physicochemical properties of drug and there was no significant difference (P < 0.05) in drug release. The response surface graph and contour plots showed the effect of variables on responses such as hardness (Y 1 ), SI (Y 4 ), and time taken for 80% of drug release (t 80% )(Y 5 ) which were found to be positively influenced by X 1 and ANOVA for response surface quadratic model was found to be significant (P < 0.0001). The FLT (Y 2 ) and TFT (Y 3 ) were found to be affected by X 2 and ANOVA for the response surface quadratic model was found to be significant (P < 0.05). Conclusion: From all the formulations, OF-8 showed ideal results in the form of hardness, FLT, TFT, SI, and time taken for 80% of drug release (t 80% ) and stability based on which it can be selected for in vivo studies.

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Formulation, Development, and Evaluation of Floating Pulsatile Drug Delivery System of Atenolol

Cited by 12 publications

References 27 publications

Characterization and Pharmacological Evaluation of Anti-Cellulite Herbal Product(s) Encapsulated in 3D-Fabricated Polymeric Microneedles

Characterization and Pharmacological Evaluation of Anti-Cellulite Herbal Product(s) Encapsulated in 3D-Fabricated Polymeric Microneedles

Pulsatile Drug Delivery: A Strategy for Treating Chronotherapeutic Ailments

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