scholarly journals Drug-Loaded Lipid-Core Micelles in Mucoadhesive Films as a Novel Dosage Form for Buccal Administration of Poorly Water-Soluble and Biological Drugs

Pharmaceutics ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 1168
Author(s):  
Wai-Houng Chou ◽  
Ariel Galaz ◽  
Miguel O. Jara ◽  
Alexander Gamboa ◽  
Javier O. Morales
Keyword(s):  
Dosage Form ◽  
Ex Vivo ◽  
Diffusion Mechanism ◽  
In Vitro Release ◽  
Water Soluble ◽  
Rhodamine 123 ◽  
Burst Release ◽  
Biological Drugs ◽  
Lipid Core ◽  
Poorly Water Soluble

The aim of the study was to develop a novel buccal dosage form to transport rhodamine 123 and human insulin as models for poorly water-soluble and biological drugs, using lipid-core micelles (LCMs)-loaded mucoadhesive films. LCMs were synthesized by a low-energy hot emulsification process, yielding spherically shaped, small-sized, monodispersed and negatively charged carriers with high entrapment efficiency. In vitro release studies demonstrated a higher release of insulin rather than rhodamine from LCMs in simulated physiological conditions, due to an initial burst release effect; however, both release profiles are mainly explained by a diffusion mechanism. Furthermore, LCMs-loaded mucoadhesive films were manufactured and preserved with similar mechanical properties and optimal mucoadhesive behavior compared to nonloaded films. Ex vivo permeation experiments using excised porcine buccal epithelium reveal that both rhodamine and insulin-loaded LCM films elicited a significantly enhanced permeation effect compared to LCMs in suspension and free drugs in solution as controls. Hence, LCMs-loaded mucoadhesive films are suitable as buccal dosage form for the transport and delivery of rhodamine 123 and insulin, as models for poorly water-soluble and biological drugs, respectively.

scholarly journals Formulation and evaluation of solid self micro emulsifying drug delivery system using aerosil 200 as solid carrier

2012 ◽  
Vol 1 (12) ◽  
pp. 414-419 ◽  
Author(s):  
Durgacharan Arun Bhagwat ◽  
John Intru D’Souza
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Intestinal Permeability ◽  
Delivery System ◽  
Ex Vivo ◽  
Water Soluble ◽  
Solid Carrier ◽  
Drug Content ◽  
Permeability Study ◽  
Poorly Water Soluble

Improvement of bio-availability of poorly water soluble drugs presents one of the furthermost challenge in drug formulations. One of the most admired and commercially viable formulation approach for this challenge is solid self micro emulsifying drug delivery system (S-SMEDDS). There are many techniques to convert liquid SMEDDS to solid, but an adsorption technique is simple and economic. Hence aim of present study was to develop S-SMEDDS of poorly water soluble drug Telmisartan (TEL) using Aerosil 200 as solid carrier. Liquid SMEDDS was prepared using Acrysol EL 135, Tween 80 and PEG 400 as oil, surfactant and co-surfactant and was converted to S-SMEDDS by adsorbing it on Aerosil 200. Prepared S-SMEDDS was evaluated for flow properties, drug content, reconstitution properties, DSC, SEM, in-vitro drug release and ex-vivo intestinal permeability study. Results showed that prepared S-SMEDDS have good flow property with 99.45 ± 0.02% drug content. Dilution study by visual observation showed that there was spontaneous micro emulsification and no sign of phase separation. Droplet size was found to be 0.34 µm with polydispersity index of 0.25. DSC thermogram showed that crystallization of TEL was inhibited. SEM photograph showed smooth surface of S-SMEDDS with less aggregation. Drug releases from S- SMEDDS were found to be significantly higher as compared with that of plain TEL. Ex-vivo intestinal permeability study revealed that diffusion of drug was significantly higher from S-SMEDDS than that of suspension of plain TEL. Study concluded that S-SMEDDS can effectively formulated by adsorption technique with enhanced dissolution rate and concomitantly bioavailability.DOI: http://dx.doi.org/10.3329/icpj.v1i12.12451 International Current Pharmaceutical Journal 2012, 1(12): 414-419

New Formulation and Evaluation of Camptothecin Encapsulated and/or Dispersed Suppository

2020 ◽  
Vol 20 ◽  
Author(s):  
Sofiane Fatmi ◽  
Lamia Taouzinet ◽  
Malika Lahiani-Skiba ◽  
Mohamed Skiba ◽  
Mokrane Iguer-Ouada
Keyword(s):  
Diffusion Mechanism ◽  
In Vitro Release ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Physical Parameters ◽  
Type I ◽  
Weight Variation ◽  
New Formulation ◽  
Soluble Base

Background: Camptothecin is known for a potent anticancer activity. However, its optimal activity is reduced due to its low solubility and stability in biological media. Objective: The aim of present study is to design and characterize a camptothecin (CPT) suppository formulation. Methods: Rectal suppositories of: camptothecin alone, encapsulated with cyclodextrin (CD) and in ternary system (CPT encapsulated with cyclodextrin and dispersed in polyethylene glycol (PEG) 6000) were prepared using various hydrophobic and hydrophilic polymeric bases as semi-synthetic glyceride (Suppocire® AM Pellets) and polyethylene glycols (PEGs) mixtures. Formulations were evaluated by various parameters like weight variation, drug content, hardness and liquefaction time. In vitro release study was performed in USP type I apparatus using phosphate buffer pH 7.2 as dissolution media. Results: Suppositories were within the permissible range of all physical parameters. In vitro drug released from water soluble base (PEG) was greater than that from oil soluble base with ninety percent (90%) of drug dissolution. It was also established that drug release from various formulations was by diffusion mechanism according to Higuchi’s equation. Conclusion: This new formulation offers a new approach to colorectal cancer treatment by offering an alternative and simple drug administration route.

REVIEW ON FAST DISSOLVING TABLET BY SOLID DISPERSION APPROACH

2021 ◽  
pp. 2840-2845
Author(s):  
V. Namitha
Keyword(s):  
Solid Dispersion ◽  
Dosage Form ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
And Performance ◽  
High Level ◽  
Determining Factor ◽  
Mouth Dissolving Tablet

Tablet is found to be the most popular dosage form among all existing dosage form. However, in certain occurrences as a result of the huge size of dosage forms, and in the uncooperative, pediatric and dysphasia patients, it might make a few problems, to avoid this issues, another type of dosage form is created, which is known as fast dissolving tablet or mouth dissolving tablet. These are the high level dosage form which breaks down within seconds when placed on the toungue. Mouth dissolving tablets have become impressive consideration as a better option in contrast to others because of better convenience to patients. This review discusses the method of preparation, properties, mechanisms; capsules to be incorporated inside the mouth dissolving pill and evaluation of the drugs are emphasized. The solid dispersion is one of the established solubilization techniques for poorly water-soluble drugs. It is basically the interaction between drug and polymer, and hence it is found to be the determining factor in its design and performance. This review additionally summarizes our knowledge on solid dispersions both in the solid as well as liquid state.

scholarly journals TECHNOLOGY DVELOPMENT FOR POLYMER MODIFICATION TO ENHANCE SOLUBILITY OF POORLY SOLUBLE DRUG

2018 ◽  
Vol 1 (1) ◽  
pp. 5-9
Author(s):  
Biresh Kumar Sarkar ◽  
Suraj Kumar Mishra ◽  
Suraj Kumar Mishra ◽  
Ajay Krishna Gupta ◽  
Shailendra S Solanki
Keyword(s):  
Dosage Form ◽  
Guar Gum ◽  
Water Soluble ◽  
Oral Dosage ◽  
In Vitro Dissolution ◽  
Polymer Modification ◽  
Water Soluble Drug ◽  
Poorly Soluble ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Solubilization of poorly soluble drugs is a frequently encountered challenge in screening studies of newchemical entities as well as in formulation design and development. Solubility of some drugs is very less; thesedrug molecules are often lipophilic and hence dissolution may be a problem in drug absorption from solid oraldosage forms. The increasing interest of the technology of dosage form with natural biopolymers has becomethe reason for undertaking present investigation on the possibility of modification of guar gum application inthe preparation of an oral solid dosage form of a poorly water soluble drug. Present study examines the effect ofmodified guar gum on the solubility of a poorly water-soluble Nevirapine. Modified guar gum was preparedusing heat treatment (110-120oC for 2 hours) method. It was characterized for viscosity and swelling index etc.The physical and co-grinding mixtures of Nevirapine with modified guar gum were prepared in 1:4 drugs togum ratio. The physical and co-grinding mixtures were characterized by DSC and FT-IR study. The studiesconfirmed that there was no interaction between drug and carrier. Prepared mixtures were evaluated forsolubility study and in vitro dissolution studies. The results of present investigation indicated that modified guargum can be a used for the development of oral dosage form with increased solubility and hence improveddissolution and oral bioavailability of poorly water soluble drug.

scholarly journals Formulation and In Vitro Evaluation of Casein Nanoparticles as Carrier for Celecoxib

2020 ◽  
Vol 10 (3) ◽  
pp. 408-417
Author(s):  
Jyotsana R. Madan ◽  
Izharahemad N. Ansari ◽  
Kamal Dua ◽  
Rajendra Awasthi
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Water Soluble ◽  
Polydispersity Index ◽  
Drug Dissolution ◽  
Permeation Studies ◽  
Poorly Water Soluble

Purpose : The objective of this work was to formulate casein (CAS) nanocarriers for the dissolution enhancement of poorly water soluble drug celecoxib (CLXB). Methods: The CLXB loaded CAS nanocarriers viz., nanoparticles, reassembled CAS micelles and nanocapsules were prepared using sodium caseinate (SOD-CAS) as a carrier to enhance the solubility of CLXB. The prepared formulations were characterized for particle size, polydispersity index, zeta potential, percentage entrapment efficiency, and surface morphology for the selection of best formulation. Fourier transform infrared spectroscopy, differential scanning calorimetry and X-ray powder diffraction study was used to for the confirmation of encapsulation of CLXB. Further, in vitro drug dissolution, ex-vivo permeation studies on chicken ileum and stability studies were carried out. Results: The CLXB loaded casein nanoparticles (CNP) (batch A2) showed a particle size diameter 216.1 nm, polydispersity index 0.422 with percentage entrapment efficiency of 90.71% and zeta potential of -24.6 mV. Scanning electron microscopy of suspension confirmed globular shape of CNP. The in vitro release data of optimized batch followed non Fickian diffusion mechanism. The ex vivo permeation studies on chicken ileum of CLXB loaded CNP showed permeation through mucous membrane as compared to pure CLXB. The apparent permeability of best selected freeze dried CLXB loaded CNP (batch A2) was higher and gradually increased from 0.90 mg/cm2 after 10 min to a maximum of 1.95 mg/cm2 over the subsequent 90 min. A higher permeation was recorded at each time point than that of the pure CLXB. Conclusion: The study explored the potential of CAS as a carrier for solubility enhancement of poorly water soluble drugs.

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